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自纳米乳化药物递送系统中的功能性辅料与新型药物递送方案:一篇评论

Functional Excipients and Novel Drug Delivery Scenario in Self-nanoemulsifying Drug Delivery System: A Critical Note.

作者信息

Tonjan Russel, Singh Dilpreet

机构信息

Department of Pharmaceutics, ISF College of Pharmacy, GT Road (NH-95), Ghal Kalan, Moga, Punjab 142001, INDIA.

出版信息

Pharm Nanotechnol. 2022 Aug 29. doi: 10.2174/2211738510666220829085745.

DOI:10.2174/2211738510666220829085745
PMID:36043758
Abstract

Lipid-based formulations have emerged as prospective dosage forms for extracting the therapeutic effects of existing lipophilic compounds and novel chemical entities more efficiently. Compared to other excipients, lipids have the added benefit of enhancing the bioavailability of lipophilic and highly metabolizable drugs due to their unique physicochemical features and similarities to in vivo components. Furthermore, lipids can minimize the needed dose and even the toxicity of drugs with poor aqueous solubility when employed as the primary excipient. Hence, the aim of the present review is to highlight the functional behavior of lipid excipients used in SNEDD formulation along with the stability aspects of the formulation in vivo. Moreover, this review also covered the importance of SNEDDS in drug delivery, the therapeutic and manufacturing benefits of lipids as excipients, and the technological advances made so far to convert liquid to solid SNEDDS like melt granulation, adsorption on solid support, spray cooling, melt extrusion/ spheronization has also highlighted. The mechanistic understanding of SNEDD absorption in vivo is highly complex, which was discussed very critically in this review. An emphasis on their application and success on an industrial scale was presented, as supported by case studies and patent surveys.

摘要

基于脂质的制剂已成为更有效地提取现有亲脂性化合物和新型化学实体治疗效果的潜在剂型。与其他辅料相比,脂质因其独特的物理化学特性以及与体内成分的相似性,具有提高亲脂性和高代谢性药物生物利用度的额外优势。此外,当用作主要辅料时,脂质可以减少所需剂量,甚至降低水溶性差的药物的毒性。因此,本综述的目的是突出用于自乳化药物递送系统(SNEDD)制剂的脂质辅料的功能行为以及该制剂在体内的稳定性方面。此外,本综述还涵盖了SNEDD在药物递送中的重要性、脂质作为辅料的治疗和制造优势,以及迄今为止在将液体SNEDD转化为固体方面取得的技术进展,如熔融制粒、吸附在固体载体上、喷雾冷却、熔融挤出/滚圆等也进行了强调。对SNEDD在体内吸收的机理理解非常复杂,本综述对此进行了非常批判性的讨论。通过案例研究和专利调查的支持,强调了它们在工业规模上的应用和成功。

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Comparison of Three Different Aqueous Microenvironments for Enhancing Oral Bioavailability of Sildenafil: Solid Self-Nanoemulsifying Drug Delivery System, Amorphous Microspheres and Crystalline Microspheres.三种不同水介质环境对提高西地那非口服生物利用度的比较:固体自微乳药物传递系统、无定形微球和结晶微球。
Int J Nanomedicine. 2021 Aug 24;16:5797-5810. doi: 10.2147/IJN.S324206. eCollection 2021.
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Self-Nanoemulsifying Drug Delivery System of Genkwanin: A Novel Approach for Anti-Colitis-Associated Colorectal Cancer.
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Drug Des Devel Ther. 2021 Feb 12;15:557-576. doi: 10.2147/DDDT.S292417. eCollection 2021.
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Current approaches in lipid-based nanocarriers for oral drug delivery.当前用于口服药物递送的基于脂质的纳米载体方法。
Drug Deliv Transl Res. 2021 Apr;11(2):471-497. doi: 10.1007/s13346-021-00908-7. Epub 2021 Feb 2.
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Formulation and in vitro evaluation of self-nanoemulsifying liquisolid tablets of furosemide.呋塞米自微乳释液体胶囊剂的处方前研究与体外评价。
Sci Rep. 2021 Jan 14;11(1):1315. doi: 10.1038/s41598-020-79940-5.
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Amino Acids. 2021 Jan;53(1):73-88. doi: 10.1007/s00726-020-02926-0. Epub 2021 Jan 4.
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