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Clinical Liposomes

文献检索行在路上发表于 2026年04月28日 09:0575阅读
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clinical liposome

Liposomes have emerged as a significant and highly adaptable therapeutic platform in clinical settings, offering distinct advantages over conventional drug delivery methods for a wide range of diseases, particularly in cancer therapy and the delivery of anti-infective agents . Their development has progressed significantly since their initial description in 1965, moving from conventional vesicles to more sophisticated "second-generation liposomes" and advanced engineered systems .

Key Characteristics and Advantages of Liposomes in Clinical Applications:

  • Biocompatibility and Biodegradability: Liposomes are formed from natural and synthetic lipids and surfactants, making them biocompatible, biodegradable, inert, and non-immunogenic. This reduces the risk of adverse reactions in patients .
  • Enhanced Drug Delivery and Efficacy: Liposomes can encapsulate both hydrophilic and hydrophobic molecules, protecting drugs from premature degradation, improving solubility, and prolonging their circulation time in the body . This leads to enhanced drug absorption and therapeutic effects while minimizing rapid clearance and systemic toxicity .
  • Targeting Capabilities: A crucial advantage of liposomes is their ability to be designed for targeted drug delivery. This can be achieved through:
    • Passive Targeting: Due to their size and surface properties, liposomes can accumulate in tumor tissues via the Enhanced Permeability and Retention (EPR) effect, where tumor vasculature is leaky and lymphatic drainage is impaired .
    • Active Targeting: Liposomes can be surface-modified with ligands (e.g., monoclonal antibodies, peptides, glycolipids, sialic acid) that bind specifically to receptors on target cells, such as tumor cells or tumor-associated stromal cells, thereby increasing selectivity and drug uptake at the desired site . This is particularly relevant for overcoming therapeutic resistance in heterogeneous tumors by targeting multiple cell subtypes simultaneously .
  • Reduced Systemic Toxicity: By preferentially delivering drugs to the site of action, liposomes reduce drug exposure to healthy tissues, leading to a decrease in systemic side effects. This is a significant benefit, especially for potent drugs like chemotherapeutics or antifungal agents .
  • Versatility in Design: The physical properties of liposomes, including composition, size, and charge, can be extensively modulated to optimize them for specific therapeutic tasks, such as prolonged blood circulation, pH responsiveness, or co-incorporation of adjuvants .

Technological Advancements Contributing to Clinical Success:

  • Long-Circulating (Stealth) Liposomes: A major breakthrough was the incorporation of poly-(ethylene glycol) (PEG) onto the liposome surface. PEGylation extends blood-circulation time by reducing uptake by the mononuclear phagocyte system (MPS) or reticuloendothelial system (RES), thereby enhancing passive targeting to tumors . Doxil®, the first FDA-approved nano-drug, utilizes PEGylated liposomes to achieve prolonged circulation and avoid RES uptake .
  • Remote Drug Loading: Techniques like remote loading, often driven by transmembrane ammonium sulfate gradients, enable high and stable encapsulation of drugs within liposomes, ensuring controlled release at the target site, as seen with Doxil® .
  • Triggered Release Liposomes: These liposomes are designed to release their cargo in response to specific stimuli (e.g., pH, temperature, ultrasound) at the disease site, further improving therapeutic precision .
  • Bioconjugation Strategies: Recent advances focus on bioconjugation to improve drug loading, targeting, and overall efficacy. This includes linking antibodies or ligands to the liposome surface for active targeting .
  • Manufacturing Innovations: While traditional liposome manufacturing can be complex, innovations like self-assembling liposome systems and microfluidic production are emerging to facilitate scalable, reproducible, and controlled production, addressing key challenges in translating laboratory-scale preparations to large-scale clinical manufacturing .

Clinical Applications and Examples:

Liposomes are an established nanomedicine delivery system with numerous products on the market and many more in the pipeline, having made a successful transition from concept to clinical application .

  • Cancer Therapy: This is a major area of liposomal application.
    • Doxil® (pegylated liposomal doxorubicin): As the first FDA-approved nano-drug (1995), Doxil® is a landmark example. It utilizes PEGylated liposomes for prolonged circulation and passive targeting to tumors through the EPR effect, leading to drug release at the tumor site and improved therapeutic outcomes compared to free doxorubicin .
    • Liposomal Irinotecan (nal-IRI): Approved for metastatic pancreatic ductal adenocarcinoma (mPDAC) previously treated with gemcitabine-based therapy. Clinical trials, such as NAPOLI-1, demonstrated that nal-IRI combined with 5-fluorouracil and leucovorin significantly improved median overall survival compared to 5-FU/LV alone . This formulation also showed advantages in progression-free survival, objective response rate, and disease control rate, with identified prognostic markers for long-term survival .
    • Chemoimmunotherapy: Liposomes are gaining attention in cancer chemoimmunotherapy to address issues of systemic toxicity and non-targeted distribution of agents. They offer a promising avenue for improving therapeutic outcomes in various malignant diseases like non-small cell lung cancer, breast cancer, and large B-cell lymphoma .
    • Colorectal Cancer (CRC): Liposomal formulations are being studied for CRC, showing improved antitumor activity, longer drug accumulation, and reduced cytotoxicity to normal cells compared to free drugs .
    • Theranostics: Engineered liposomal nanoparticles are also used in cancer theranostics, combining therapeutic and imaging agents for image-guided therapies and combination treatments. Nanosized liposomes can deliver multiple agents to target sites in solid tumors, although integrating these probes without compromising performance is a challenge . Surface engineering has been shown to improve tumor selectivity, therapeutic activity, and retention .
  • Anti-fungal and Antibiotic Drugs:
    • Liposomal Amphotericin B: Discovered in the 1950s, this polyene antifungal compound formulated as a liposomal drug delivery system has been used for decades to treat systemic fungal infections (e.g., Aspergillus, cryptococcal disease, Candida infections) and visceral leishmaniasis. The liposomal formulation significantly improved the therapeutic index by allowing higher drug concentrations in plasma and tissue while simultaneously lowering toxicity compared to amphotericin B deoxycholate .
  • Vaccines: Liposomes have a long history as vehicles for antigen delivery in vaccines. They can carry both membrane-associated and water-soluble antigens, and their customizable properties allow for optimized design for specific tasks, including co-incorporation of adjuvants. Registered liposomal vaccines exist, and clinical trials for new formulations are ongoing .
  • Anesthetics and Anti-inflammatory Drugs: Liposomes are also being explored for the delivery of anesthetics and anti-inflammatory drugs, indicating their broad applicability beyond oncology and anti-infectives .
  • Gene Medicines: Liposomes are used to deliver nucleic acid polymers, contributing to the development of gene therapies .

Challenges and Future Directions:

Despite significant progress and numerous successful clinical applications, several challenges remain in the full clinical translation and widespread adoption of liposomal drug delivery systems:

  • Scale-Up and Manufacturing: Scaling up production and comprehensive characterization of ligand-functionalized liposome formulations remains a challenge. Laboratory-scale preparation methods often do not translate easily to large-scale, cost-effective manufacturing, which can delay the development of new liposomal systems . Innovations in manufacturing processes, such as microfluidics and self-assembling systems, are crucial for overcoming these hurdles .
  • Stability and Reproducibility: Liposomal systems can suffer from fragility, premature leakage of loaded cargo, and issues with reproducibility, which affect their stability and smooth circulation in vivo .
  • Targeting Specificity: While active targeting offers greater selectivity, achieving precise, site-selective tumor targeting without compromising biodistribution is still an area of active research . Preclinical models often inadequately recapitulate the complexity of in vivo tumors, leading to challenges in translating promising results of ligand-directed liposomes to clinical success .
  • Immunogenicity and Toxicity: Although generally biocompatible, the use of certain components, particularly PEG, has raised concerns about potential immunogenicity (e.g., anti-PEG antibodies) and accelerated blood clearance in some cases, which could impact the efficacy of subsequent doses . Toxicity to vital organs must also be carefully addressed .
  • Regulatory Pathways: The regulatory landscape for nanomedicines, including liposomes, is evolving. Clearer guidance and established methods for characterization are needed to streamline the approval process for novel liposomal products and their generic counterparts . The absence of FDA-approved generic Doxil®, years after its patents expired, highlights the complexities and lessons learned in this regard .
  • Translational Gaps: Despite encouraging preclinical results for many novel liposomal formulations, including immunoliposomes (antibody-conjugated liposomes designed for selective targeting), their clinical translation has been limited . More efforts are warranted to bridge the gap between preclinical success and clinical application .

Conclusion:

Liposomes represent a cornerstone of nanomedicine, having demonstrated their utility and versatility as drug delivery systems in numerous clinical applications. Their ability to improve drug pharmacokinetics, enhance therapeutic efficacy, and reduce toxicity has made them invaluable, particularly in oncology and infectious disease treatment. Ongoing research and innovation in liposome design, targeting strategies, and manufacturing processes are continuously expanding their potential, promising a future with more advanced and effective liposomal therapies . Addressing current challenges in scale-up, stability, and clinical translation will be key to unlocking the full potential of this established and evolving technology.

References

1Stealth liposomes: review of the basic science, rationale, and clinical applications, existing and potential.PubMed

Maria Laura Immordino, Franco Dosio, Luigi Cattel
Int J Nanomedicine. 2006;1(3):297-315.
Among several promising new drug-delivery systems, liposomes represent an advanced technology to deliver active molecules to the site of action, and at present several formulations are in clinical use. Research on liposome technology has progressed from conventional vesicles ("first-generation liposomes") to "second-generation liposomes", in which long-circulating liposomes are obtained by modulating the lipid composition, size, and charge of the vesicle. Liposomes with modified surfaces have also been developed using several molecules, such as glycolipids or sialic acid. A significant step in the development of long-circulating liposomes came with inclusion of the synthetic polymer poly-(ethylene glycol) (PEG) in liposome composition. The presence of PEG on the surface of the liposomal carrier has been shown to extend blood-circulation time while reducing mononuclear phagocyte system uptake (stealth liposomes). This technology has resulted in a large number of liposome formulations encapsulating active molecules, with high target efficiency and activity. Further, by synthetic modification of the terminal PEG molecule, stealth liposomes can be actively targeted with monoclonal antibodies or ligands. This review focuses on stealth technology and summarizes pre-clinical and clinical data relating to the principal liposome formulations; it also discusses emerging trends of this promising technology.

2Doxil®--the first FDA-approved nano-drug: lessons learned.PubMed

Yechezkel Barenholz
J Control Release. 2012 Jun 10;160(2):117-34. doi: 10.1016/j.jconrel.2012.03.020. Epub 2012 Mar 29.
Doxil®, the first FDA-approved nano-drug (1995), is based on three unrelated principles: (i) prolonged drug circulation time and avoidance of the RES due to the use of PEGylated nano-liposomes; (ii) high and stable remote loading of doxorubicin driven by a transmembrane ammonium sulfate gradient, which also allows for drug release at the tumor; and (iii) having the liposome lipid bilayer in a "liquid ordered" phase composed of the high-T(m) (53 °C) phosphatidylcholine, and cholesterol. Due to the EPR effect, Doxil is "passively targeted" to tumors and its doxorubicin is released and becomes available to tumor cells by as yet unknown means. This review summarizes historical and scientific perspectives of Doxil development and lessons learned from its development and 20 years of its use. It demonstrates the obligatory need for applying an understanding of the cross talk between physicochemical, nano-technological, and biological principles. However, in spite of the large reward, ~2 years after Doxil-related patents expired, there is still no FDA-approved generic "Doxil" available.

3Liposome composition in drug delivery design, synthesis, characterization, and clinical application.PubMed

Danielle E Large, Rudolf G Abdelmessih, Elizabeth A Fink, et al.
Adv Drug Deliv Rev. 2021 Sep;176:113851. doi: 10.1016/j.addr.2021.113851. Epub 2021 Jul 2.
Liposomal drug delivery represents a highly adaptable therapeutic platform for treating a wide range of diseases. Natural and synthetic lipids, as well as surfactants, are commonly utilized in the synthesis of liposomal drug delivery vehicles. The molecular diversity in the composition of liposomes enables drug delivery with unique physiological functions, such as pH response, prolonged blood circulation, and reduced systemic toxicity. Herein, we discuss the impact of composition on liposome synthesis, function, and clinical utility.

4Liposomes and ISCOMs.PubMed

Gideon F A Kersten, Daan J A Crommelin
Vaccine. 2003 Feb 14;21(9-10):915-20. doi: 10.1016/s0264-410x(02)00540-6.
Liposomes and ISCOMs have a long history as vehicles for antigen delivery. Liposomes can carry both membrane associated antigens as well as water soluble molecules. Their physical properties are highly variable, depending on composition and manufacturing method. This allows optimised design for specific tasks (targeting, co-incorporation of adjuvants, etc.). ISCOMs already have a build-in adjuvant, Quillaja saponin, which is a structural part of the vehicle. In recent years, considerable progress has been achieved with respect to the use of better defined saponin. Clinical trials with ISCOMs are in progress and registered liposomal vaccines exist. Here, follows a brief overview on recent developments with emphasis on pharmaceutical aspects.

5Towards clinical translation of ligand-functionalized liposomes in targeted cancer therapy: Challenges and opportunities.PubMed

Lisa Belfiore, Darren N Saunders, Marie Ranson, et al.
J Control Release. 2018 May 10;277:1-13. doi: 10.1016/j.jconrel.2018.02.040. Epub 2018 Mar 1.
The development of therapeutic resistance to targeted anticancer therapies remains a significant clinical problem, with intratumoral heterogeneity playing a key role. In this context, improving the therapeutic outcome through simultaneous targeting of multiple tumor cell subtypes within a heterogeneous tumor is a promising approach. Liposomes have emerged as useful drug carriers that can reduce systemic toxicity and increase drug delivery to the tumor site. While clinically used liposomal drug formulations show marked therapeutic advantages over free drug formulations, ligand-functionalized liposomes that can target multiple tumor cell subtypes may further improve the therapeutic efficacy by facilitating drug delivery to a broader population of tumor cells making up the heterogeneous tumor tissue. Ligand-directed liposomes enable the so-called active targeting of cell receptors via surface-attached ligands that direct drug uptake into tumor cells or tumor-associated stromal cells, and so can increase the selectivity of drug delivery. Despite promising preclinical results demonstrating improved targeting and anti-tumor effects of ligand-directed liposomes, there has been limited translation of this approach to the clinic. Key challenges for translation include the lack of established methods to scale up production and comprehensively characterize ligand-functionalized liposome formulations, as well as the inadequate recapitulation of in vivo tumors in the preclinical models currently used to evaluate their performance. Herein, we discuss the utility of recent ligand-directed liposome approaches, with a focus on dual-ligand liposomes, for the treatment of solid tumors and examine the drawbacks limiting their progression to clinical adoption.

6Liposomal drug delivery systems: from concept to clinical applications.PubMed

Theresa M Allen, Pieter R Cullis
Adv Drug Deliv Rev. 2013 Jan;65(1):36-48. doi: 10.1016/j.addr.2012.09.037. Epub 2012 Oct 1.
The first closed bilayer phospholipid systems, called liposomes, were described in 1965 and soon were proposed as drug delivery systems. The pioneering work of countless liposome researchers over almost 5 decades led to the development of important technical advances such as remote drug loading, extrusion for homogeneous size, long-circulating (PEGylated) liposomes, triggered release liposomes, liposomes containing nucleic acid polymers, ligand-targeted liposomes and liposomes containing combinations of drugs. These advances have led to numerous clinical trials in such diverse areas as the delivery of anti-cancer, anti-fungal and antibiotic drugs, the delivery of gene medicines, and the delivery of anesthetics and anti-inflammatory drugs. A number of liposomes (lipidic nanoparticles) are on the market, and many more are in the pipeline. Lipidic nanoparticles are the first nanomedicine delivery system to make the transition from concept to clinical application, and they are now an established technology platform with considerable clinical acceptance. We can look forward to many more clinical products in the future.

7Recent Progress in Bioconjugation Strategies for Liposome-Mediated Drug Delivery.PubMed

Bethany Almeida, Okhil K Nag, Katherine E Rogers, et al.
Molecules. 2020 Dec 1;25(23):5672. doi: 10.3390/molecules25235672.
In nanoparticle (NP)-mediated drug delivery, liposomes are the most widely used drug carrier, and the only NP system currently approved by the FDA for clinical use, owing to their advantageous physicochemical properties and excellent biocompatibility. Recent advances in liposome technology have been focused on bioconjugation strategies to improve drug loading, targeting, and overall efficacy. In this review, we highlight recent literature reports (covering the last five years) focused on bioconjugation strategies for the enhancement of liposome-mediated drug delivery. These advances encompass the improvement of drug loading/incorporation and the specific targeting of liposomes to the site of interest/drug action. We conclude with a section highlighting the role of bioconjugation strategies in liposome systems currently being evaluated for clinical use and a forward-looking discussion of the field of liposomal drug delivery.

8Sonothrombolysis.PubMed

Stephen Meairs
Front Neurol Neurosci. 2015;36:83-93. doi: 10.1159/000366239. Epub 2014 Dec 22.
Ultrasound (US) applied as an adjunct to thrombolytic therapy improves the recanalization of occluded vessels, and microbubbles can amplify this effect. New data suggests that the combination of US and microbubbles without tissue plasminogen activator may achieve recanalization with a lower risk of hemorrhage. Further possibilities include specific targeting of thrombus with immunobubbles as well as local drug delivery with US-sensitive liposomes. Clinical studies support the use of US for ischemic stroke therapy, and the first trials of enhancing sonothrombolysis with microbubbles have been encouraging. One emerging clinical application is sonothrombolysis of intracranial hemorrhages for clot evacuation. Microcirculation, irrespective of recanalization, may also be improved by US and microbubbles, and this effect may open new opportunities for the application of sonothrombolysis in acute ischemic stroke. Understanding the mechanisms of therapeutic action and relating this knowledge to issues of efficacy and safety are important objectives of ongoing research. This review will discuss the translational capacities of in vitro studies and preclinical research and will assess the first clinical studies of this promising therapeutic strategy.

9Engineered Liposomes in Interventional Theranostics of Solid Tumors.PubMed

Nagavendra Kommineni, Ruchita Chaudhari, João Conde, et al.
ACS Biomater Sci Eng. 2023 Aug 14;9(8):4527-4557. doi: 10.1021/acsbiomaterials.3c00510. Epub 2023 Jul 14.
Engineered liposomal nanoparticles have unique characteristics as cargo carriers in cancer care and therapeutics. Liposomal theranostics have shown significant progress in preclinical and clinical cancer models in the past few years. Liposomal hybrid systems have not only been approved by the FDA but have also reached the market level. Nanosized liposomes are clinically proven systems for delivering multiple therapeutic as well as imaging agents to the target sites in (i) cancer theranostics of solid tumors, (ii) image-guided therapeutics, and (iii) combination therapeutic applications. The choice of diagnostics and therapeutics can intervene in the theranostics property of the engineered system. However, integrating imaging and therapeutics probes within lipid self-assembly "liposome" may compromise their overall theranostics performance. On the other hand, liposomal systems suffer from their fragile nature, site-selective tumor targeting, specific biodistribution and premature leakage of loaded cargo molecules before reaching the target site. Various engineering approaches, viz., grafting, conjugation, encapsulations, etc., have been investigated to overcome the aforementioned issues. It has been studied that surface-engineered liposomes demonstrate better tumor selectivity and improved therapeutic activity and retention in cells/or solid tumors. It should be noted that several other parameters like reproducibility, stability, smooth circulation, toxicity of vital organs, patient compliance, etc. must be addressed before using liposomal theranostics agents in solid tumors or clinical models. Herein, we have reviewed the importance and challenges of liposomal medicines in targeted cancer theranostics with their preclinical and clinical progress and a translational overview.

10NAPOLI-1 phase 3 study of liposomal irinotecan in metastatic pancreatic cancer: Final overall survival analysis and characteristics of long-term survivors.PubMed

Andrea Wang-Gillam, Richard A Hubner, Jens T Siveke, et al.
Eur J Cancer. 2019 Feb;108:78-87. doi: 10.1016/j.ejca.2018.12.007. Epub 2019 Jan 14.
BACKGROUND: Liposomal irinotecan (nal-IRI) plus 5-fluorouracil and leucovorin (5-FU/LV) is approved for patients with metastatic pancreatic ductal adenocarcinoma (mPDAC) previously treated with gemcitabine-based therapy. This approval was based on significantly improved median overall survival compared with 5-FU/LV alone (6.1 vs 4.2 months; hazard ratio [HR], 0.67) in the global phase 3 NAPOLI-1 trial. Here, we report the final survival analysis and baseline characteristics associated with long-term survivors (survival of ≥1 year) in the NAPOLI-1 trial. PATIENTS AND METHODS: Patients with mPDAC were randomised to receive nal-IRI + 5-FU/LV (n = 117), nal-IRI (n = 151), or 5-FU/LV (n = 149) for the first 4 weeks of 6-week cycles. Baseline characteristics and efficacy in the overall population were compared with those in patients who survived ≥1 year. Through 16th November 2015, 382 overall survival events had occurred. RESULTS: The overall survival advantage for nal-IRI+5-FU/LV vs 5-FU/LV was maintained from the original nanoliposomal irinotecan with fluorouracil and folinic acid in metastatic pancreatic cancer after previous gemcitabine-based therapy (NAPOLI-1) analysis (6.2 vs 4.2 months, respectively; HR, 0.75; 95% confidence interval: 0.57-0.99). Median progression-free survival, objective response rate and disease control rate also favoured nal-IRI+5-FU/LV therapy. Estimated one-year overall survival rates were 26% with nal-IRI+5-FU/LV and 16% with 5-FU/LV. Baseline characteristics associated with long-term survival in the nal-IRI+5-FU/LV arm were Karnofsky performance status ≥90, age ≤65 years, lower CA19-9 levels, neutrophil-to-lymphocyte ratio ≤5 and no liver metastases. No new safety concerns were detected. CONCLUSIONS: The survival benefits of nal-IRI+5-FU/LV versus 5-FU/LV were maintained over an extended follow-up, and prognostic markers of survival ≥1 year were identified. CLINICAL TRIAL REGISTRATION NUMBER: NCT01494506.

11Liposomes-enabled cancer chemoimmunotherapy.PubMed

Lele Zhang, Jiangpei Shi, Mao-Hua Zhu, et al.
Biomaterials. 2025 Feb;313:122801. doi: 10.1016/j.biomaterials.2024.122801. Epub 2024 Sep 3.
Chemoimmunotherapy is an emerging paradigm in the clinic for treating several malignant diseases, such as non-small cell lung cancer, breast cancer, and large B-cell lymphoma. However, the efficacy of this strategy is still restricted by serious adverse events and a high therapeutic termination rate, presumably due to the lack of tumor-targeted distribution of both chemotherapeutic and immunotherapeutic agents. Targeted drug delivery has the potential to address this issue. Among the most promising nanocarriers in clinical translation, liposomes have drawn great attention in cancer chemoimmunotherapy in recent years. Liposomes-enabled cancer chemoimmunotherapy has made significant progress in clinics, with impressive therapeutic outcomes. This review summarizes the latest preclinical and clinical progress in liposome-enabled cancer chemoimmunotherapy and discusses the challenges and future directions of this field.

12Liposomes: Advancements and innovation in the manufacturing process.PubMed

Sanket Shah, Vivek Dhawan, René Holm, et al.
Adv Drug Deliv Rev. 2020;154-155:102-122. doi: 10.1016/j.addr.2020.07.002. Epub 2020 Jul 8.
Liposomes are well recognised as effective drug delivery systems, with a range of products approved, including follow on generic products. Current manufacturing processes used to produce liposomes are generally complex multi-batch processes. Furthermore, liposome preparation processes adopted in the laboratory setting do not offer easy translation to large scale production, which may delay the development and adoption of new liposomal systems. To promote advancement and innovation in liposome manufacturing processes, this review considers the range of manufacturing processes available for liposomes, from laboratory scale and scale up, through to large-scale manufacture and evaluates their advantages and limitations. The regulatory considerations associated with the manufacture of liposomes is also discussed. New innovations that support leaner scalable technologies for liposome fabrication are outlined including self-assembling liposome systems and microfluidic production. The critical process attributes that impact on the liposome product attributes are outlined to support potential wider adoption of these innovations.

13New Trends in Liposome-based Drug Delivery in Colorectal Cancer.PubMed

Julia B Krajewska, Adrian Bartoszek, Jakub Fichna
Mini Rev Med Chem. 2019;19(1):3-11. doi: 10.2174/1389557518666180903150928.
Colorectal cancer (CRC) is one of the most common cancers in both men and women. Approximately one-third of patients do not survive five years from diagnosis, which indicates the need for treatment improvement, also through new ways of drug delivery. A possible strategy to increase treatment efficacy is the use of liposomal formulation, which allows delivering both hydrophobic and hydrophilic compounds with better biocompatibility and reduced side-effects. Liposomal formulations showed better antitumor activity, longer drug accumulation and no cytotoxic effect on normal cells when compared to free drugs. In this review, we will present liposomal preparations studied in CRC in vitro and in vivo. We will focus on the advantages of liposomal delivery over conventional therapy as well as modifications which increase specificity, drug accumulation and efficacy. Moreover, we will discuss formulations investigated in clinical trials. Liposomal delivery has a great potential in overcoming current limitations of cancer therapy and development of this system gives new perspectives in CRC treatment.

14Liposomal amphotericin B-the past.PubMed

R J Brüggemann, G M Jensen, C Lass-Flörl
J Antimicrob Chemother. 2022 Nov 25;77(Suppl_2):ii3-ii10. doi: 10.1093/jac/dkac351.
The discovery of amphotericin B, a polyene antifungal compound, in the 1950s, and the formulation of this compound in a liposomal drug delivery system, has resulted in decades of use in systemic fungal infections. The use of liposomal amphotericin B formulation is referenced in many international guidelines for the treatment of fungal infections such as Aspergillus and cryptococcal disease and Candida infections, as well as other less common infections such as visceral leishmaniasis. With the development of liposomal amphotericin B, an improved therapeutic index could be achieved that allowed the attainment of higher drug concentrations in both the plasma and tissue while simultaneously lowering the toxicity compared with amphotericin B deoxycholate. In over 30 years of experience with this drug, a vast amount of information has been collected on preclinical and clinical efficacy against a wide variety of pathogens, as well as evidence on its toxicity. This article explores the history and nature of the liposomal formulation, the key clinical studies that developed the pharmacokinetic, safety and efficacy profile of the liposomal formulation, and the available microbiological data.

15Nano-based drug delivery system for therapeutics: a comprehensive review.PubMed

Satyendra Prakash
Biomed Phys Eng Express. 2023 Aug 17;9(5). doi: 10.1088/2057-1976/acedb2.
Nanomedicine and nano-delivery systems hold unlimited potential in the developing sciences, where nanoscale carriers are employed to efficiently deliver therapeutic drugs at specifically targeted sites in a controlled manner, imparting several advantages concerning improved efficacy and minimizing adverse drug reactions. These nano-delivery systems target-oriented delivery of drugs with precision at several site-specific, with mild toxicity, prolonged circulation time, high solubility, and long retention time in the biological system, which circumvent the problems associated with the conventional delivery approach. Recently, nanocarriers such as dendrimers, liposomes, nanotubes, and nanoparticles have been extensively investigated through structural characteristics, size manipulation, and selective diagnosis through disease imaging molecules, which are very effective and introduce a new paradigm shift in drugs. In this review, the use of nanomedicines in drug delivery has been demonstrated in treating various diseases with significant advances and applications in different fields. In addition, this review discusses the current challenges and future directions for research in these promising fields as well.

16Liposomes: Clinical Applications and Potential for Image-Guided Drug Delivery.PubMed

Narottam Lamichhane, Thirupandiyur S Udayakumar, Warren D D'Souza, et al.
Molecules. 2018 Jan 30;23(2):288. doi: 10.3390/molecules23020288.
Liposomes have been extensively studied and are used in the treatment of several diseases. Liposomes improve the therapeutic efficacy by enhancing drug absorption while avoiding or minimizing rapid degradation and side effects, prolonging the biological half-life and reducing toxicity. The unique feature of liposomes is that they are biocompatible and biodegradable lipids, and are inert and non-immunogenic. Liposomes can compartmentalize and solubilize both hydrophilic and hydrophobic materials. All these properties of liposomes and their flexibility for surface modification to add targeting moieties make liposomes more attractive candidates for use as drug delivery vehicles. There are many novel liposomal formulations that are in various stages of development, to enhance therapeutic effectiveness of new and established drugs that are in preclinical and clinical trials. Recent developments in multimodality imaging to better diagnose disease and monitor treatments embarked on using liposomes as diagnostic tool. Conjugating liposomes with different labeling probes enables precise localization of these liposomal formulations using various modalities such as PET, SPECT, and MRI. In this review, we will briefly review the clinical applications of liposomal formulation and their potential imaging properties.

17A Review of Liposomes as a Drug Delivery System: Current Status of Approved Products, Regulatory Environments, and Future Perspectives.PubMed

Peng Liu, Guiliang Chen, Jingchen Zhang
Molecules. 2022 Feb 17;27(4):1372. doi: 10.3390/molecules27041372.
Liposomes have been considered promising and versatile drug vesicles. Compared with traditional drug delivery systems, liposomes exhibit better properties, including site-targeting, sustained or controlled release, protection of drugs from degradation and clearance, superior therapeutic effects, and lower toxic side effects. Given these merits, several liposomal drug products have been successfully approved and used in clinics over the last couple of decades. In this review, the liposomal drug products approved by the U.S. Food and Drug Administration (FDA) and European Medicines Agency (EMA) are discussed. Based on the published approval package in the FDA and European public assessment report (EPAR) in EMA, the critical chemistry information and mature pharmaceutical technologies applied in the marketed liposomal products, including the lipid excipient, manufacturing methods, nanosizing technique, drug loading methods, as well as critical quality attributions (CQAs) of products, are introduced. Additionally, the current regulatory guidance and future perspectives related to liposomal products are summarized. This knowledge can be used for research and development of the liposomal drug candidates under various pipelines, including the laboratory bench, pilot plant, and commercial manufacturing.

18Clinical translation of immunoliposomes for cancer therapy: recent perspectives.PubMed

Di Wang, Yating Sun, Yange Liu, et al.
Expert Opin Drug Deliv. 2018 Sep;15(9):893-903. doi: 10.1080/17425247.2018.1517747. Epub 2018 Sep 12.
INTRODUCTION: Liposomes have been extensively investigated as drug delivery vehicles. Immunoliposomes (ILs) are antibody-conjugated liposomes designed to selectively target antigen-expressing cells. ILs can be used to deliver drugs to tumor cells for improving efficacy and reducing toxicity. In addition, ILs can be used in immunoassays, immunotherapy, and imaging. Although there has been extensive coverage on ILs in the literature, only a limited number of clinical trials have been reported and no IL drug has been approved by the FDA. AREAS COVERED: Factors to consider in developing ILs are discussed, including the choice of antibody or antibody fragment, the formulation of liposomes, and the conjugation chemistry. In addition, challenges and opportunities in clinical development of ILs are discussed. The purpose of this review is to provide an overview on the state of the art of ILs and to discuss potential future developments. EXPERT OPINION: IL research has had a lengthy history and numerous preclinical studies have yielded encouraging results. However, there are a number of obstacles to clinical translation of ILs. Given the unique capabilities of ILs, its potential for clinical application is underexplored. There is great potential for expanded role for ILs in the clinic and further efforts to this end are warranted. ABBREVIATIONS: Ab: antibody; ADCs: antibody-drug conjugates; API: active pharmaceutical ingredient; ADCC: antibody-dependent cellular cytotoxicity; CR: complete remission; cGMP: current good manufacturing practice; DSPE: distearoyl phosphatidylethanolamine; EGF: epidermal growth factor; EGFR: epidermal growth factor receptor; EPR: enhanced permeability and retention; Fc: fragment crystalline; Tf: transferrin; HACA: human-anti-chimeric antibody; HAHA: human-anti-human antibody; HAMA: human-anti-mouse antibody; HER2: human epidermal growth factor 2; IL: immunoliposome; LNPs: lipid nanoparticles; MRI: magnetic resonance imaging; MTD: maximum tolerated dose; PEG: polyethylene glycol; PET: positron emission tomography; PR: partial response; PSMA: prostate-specific membrane antigen; scFv: single-chain variable fragment; SPECT: single photon emission computed tomography; TTR: transthyretin.

19Chemical Advances in Therapeutic Application of Exosomes and Liposomes.PubMed

Boon Cheng Chew, Fong Fong Liew, Hsiao Wei Tan, et al.
Curr Med Chem. 2022;29(25):4445-4473. doi: 10.2174/0929867329666220221094044.
Exosomes and liposomes are vesicular nanoparticles that can encapsulate functional cargo. The chemical similarities between naturally occurring exosomes and synthetic liposomes have accelerated the development of exosome mimetics as a therapeutic drug delivery platform under physiological and pathological environments. To maximise the applications of exosomes and liposomes in the clinical setting, it is essential to look into their basic chemical properties and utilise these characteristics to optimise the preparation, loading, modification and hybridisation. This review summarises the chemical and biological properties of both exosomal and liposomal systems as well as some of the challenges related to their production and application. This article concludes with a discussion on potential perspectives for the integration of exosomal and liposomal technologies in mapping better approaches for their biomedical use, especially in therapeutics.

20Cancer theranostic applications of lipid-based nanoparticles.PubMed

Wei-Lun Tang, Wei-Hsin Tang, Shyh-Dar Li
Drug Discov Today. 2018 May;23(5):1159-1166. doi: 10.1016/j.drudis.2018.04.007. Epub 2018 Apr 13.
A variety of nanoplatforms have been developed and applied for cancer therapy, imaging, or the combination thereof. These nanoplatforms, combined with therapeutic and imaging functionalities, display great potential to enhance medical care. In particular, lipid-based nanoparticles (LNPs) are among the most-studied platforms that have resulted in many encouraging advances in theranostics. LNPs are biodegradable and biocompatible, and their formulation can be tailored for various applications. Here, we provide an overview of recent developments of four representative LNP platforms for theranostics: stealth liposomes, triggered-release liposomes, porphysomes, and lipid-coated calcium phosphate NPs (LCPs). We discuss their potential, limitations, and potential applications for cancer care and highlight perspectives and future directions for the nanotheranostics field.
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