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Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs.

作者信息

Kumari Lakshmi, Choudhari Yash, Patel Preeti, Gupta Ghanshyam Das, Singh Dilpreet, Rosenholm Jessica M, Bansal Kuldeep Kumar, Kurmi Balak Das

机构信息

Department of Pharmaceutics, ISF College of Pharmacy, GT Road, Moga 142001, Punjab, India.

Department of Pharmaceutical Chemistry, ISF College of Pharmacy, GT Road, Moga 142001, Punjab, India.

出版信息

Life (Basel). 2023 Apr 27;13(5):1099. doi: 10.3390/life13051099.


DOI:10.3390/life13051099
PMID:37240744
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10221903/
Abstract

A drug's aqueous solubility is defined as the ability to dissolve in a particular solvent, and it is currently a major hurdle in bringing new drug molecules to the market. According to some estimates, up to 40% of commercialized products and 70-90% of drug candidates in the development stage are poorly soluble, which results in low bioavailability, diminished therapeutic effects, and dosage escalation. Because of this, solubility must be taken into consideration when developing and fabricating pharmaceutical products. To date, a number of approaches have been investigated to address the problem of poor solubility. This review article attempts to summarize several conventional methods utilized to increase the solubility of poorly soluble drugs. These methods include the principles of physical and chemical approaches such as particle size reduction, solid dispersion, supercritical fluid technology, cryogenic technology, inclusion complex formation techniques, and floating granules. It includes structural modification (i.e., prodrug, salt formation, co-crystallization, use of co-solvents, hydrotrophy, polymorphs, amorphous solid dispersions, and pH variation). Various nanotechnological approaches such as liposomes, nanoparticles, dendrimers, micelles, metal organic frameworks, nanogels, nanoemulsions, nanosuspension, carbon nanotubes, and so forth have also been widely investigated for solubility enhancement. All these approaches have brought forward the enhancement of the bioavailability of orally administered drugs by improving the solubility of poorly water-soluble drugs. However, the solubility issues have not been completely resolved, owing to several challenges associated with current approaches, such as reproducibility in large scale production. Considering that there is no universal approach for solving solubility issues, more research is needed to simplify the existing technologies, which could increase the number of commercially available products employing these techniques.

摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/bdcf919a250b/life-13-01099-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/c6590457c78b/life-13-01099-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/4fae64cbda05/life-13-01099-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/7da1ed9389c7/life-13-01099-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/2db904d33293/life-13-01099-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/1ae92ba8352e/life-13-01099-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/bdcf919a250b/life-13-01099-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/c6590457c78b/life-13-01099-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/4fae64cbda05/life-13-01099-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/7da1ed9389c7/life-13-01099-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/2db904d33293/life-13-01099-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/1ae92ba8352e/life-13-01099-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1af/10221903/bdcf919a250b/life-13-01099-g006.jpg

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本文引用的文献

[1]
Validation of a Novel Supercritical Fluid Extractor/Dryer Combo Instrument.

Assay Drug Dev Technol. 2023-4

[2]
Preparation of Doxorubicin Liposomes by Remote Loading Method.

Methods Mol Biol. 2023

[3]
Functional block copolymer micelles based on poly (jasmine lactone) for improving the loading efficiency of weakly basic drugs.

RSC Adv. 2022-9-21

[4]
Bioavailability Enhancement Techniques for Poorly Aqueous Soluble Drugs and Therapeutics.

Biomedicines. 2022-8-23

[5]
Functionalized carbon nanotubes: synthesis, properties and applications in water purification, drug delivery, and material and biomedical sciences.

Nanoscale Adv. 2021-8-9

[6]
Off-Stoichiometric Thiol-Ene Chemistry to Dendritic Nanogel Therapeutics.

Adv Funct Mater. 2019-5-2

[7]
Supercritical fluid technology for solubilization of poorly water soluble drugs via micro- and naonosized particle generation.

ADMET DMPK. 2020-6-29

[8]
Curcumin Delivery on Metal-Organic Frameworks: The Effect of the Metal Center on Pharmacokinetics within the M-MOF-74 Family.

ACS Appl Bio Mater. 2021-4-19

[9]
Encapsulating quercetin in cyclodextrin metal-organic frameworks improved its solubility and bioavailability.

J Sci Food Agric. 2022-7

[10]
Multifunctional Polymeric Nanogels for Biomedical Applications.

Gels. 2021-11-23

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