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泊洛沙姆混合物混合胶束凝胶用于改善难溶性布洛芬的增溶作用及用作热敏原位凝胶

Mixed Micellar Gel of Poloxamer Mixture for Improved Solubilization of Poorly Water-Soluble Ibuprofen and Use as Thermosensitive In Situ Gel.

作者信息

Hirun Namon, Kraisit Pakorn, Santhan Supaporn

机构信息

Thammasat University Research Unit in Smart Materials and Innovative Technology for Pharmaceutical Applications (SMIT-Pharm), Faculty of Pharmacy, Thammasat University, Pathumthani 12120, Thailand.

出版信息

Pharmaceutics. 2024 Aug 10;16(8):1055. doi: 10.3390/pharmaceutics16081055.

DOI:10.3390/pharmaceutics16081055
PMID:39204400
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11359337/
Abstract

The aqueous solution of binary mixtures of amphiphilic copolymers is a potential platform for fabricating mixed polymeric micelles for pharmaceutical applications, particularly in developing drug delivery depots for a poorly water-soluble compound. This study fabricated and investigated binary mixtures of poloxamer 403 (P403) and poloxamer 407 (P407) at varying P403:P407 molar ratios to develop a vehicle for the poorly water-soluble compound, using ibuprofen as a model drug. The cooperative formation of mixed micelles was obtained, and the solubility of ibuprofen in the binary mixtures was enhanced compared to the solubility in pure water and an aqueous single P407 solution. The binary mixture with the P403:P407 molar ratio of 0.75:0.25 at a total polymer concentration of 19% / exhibited the temperature dependence of micellization and sol-to-gel characteristics of the thermosensitive mixed micellar gels. It possessed suitable micellization and gelation characteristics for in situ gelling systems. The release of ibuprofen from the thermosensitive mixed micellar depots was sustained through a diffusion-controlled mechanism. The findings can aid in formulating binary mixtures of P403 and P407 to achieve the desired properties of mixed micelles and micellar gels.

摘要

两亲性共聚物二元混合物的水溶液是制备用于药物应用的混合聚合物胶束的潜在平台，特别是在开发难溶性化合物的药物递送库方面。本研究制备并研究了泊洛沙姆403（P403）和泊洛沙姆407（P407）在不同P403:P407摩尔比下的二元混合物，以开发一种用于难溶性化合物的载体，使用布洛芬作为模型药物。获得了混合胶束的协同形成，与在纯水中和单一P407水溶液中的溶解度相比，布洛芬在二元混合物中的溶解度有所提高。在总聚合物浓度为19%时，P403:P407摩尔比为0.75:0.25的二元混合物表现出胶束化的温度依赖性和热敏性混合胶束凝胶的溶胶-凝胶特性。它具有适合原位凝胶系统的胶束化和凝胶化特性。布洛芬从热敏性混合胶束库中的释放是通过扩散控制机制持续进行的。这些发现有助于配制P403和P407的二元混合物，以实现混合胶束和胶束凝胶的所需特性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/65a84fb5096d/pharmaceutics-16-01055-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/0e7b8f01bca0/pharmaceutics-16-01055-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/16a5c9cc19e7/pharmaceutics-16-01055-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/00f468761ebb/pharmaceutics-16-01055-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/6798360ce50b/pharmaceutics-16-01055-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/5ed362d4200b/pharmaceutics-16-01055-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/d39f09000d65/pharmaceutics-16-01055-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/ae705f11e9c0/pharmaceutics-16-01055-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/07b659212456/pharmaceutics-16-01055-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/5dfe40ab92b1/pharmaceutics-16-01055-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/de3fbe1b277f/pharmaceutics-16-01055-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/65a84fb5096d/pharmaceutics-16-01055-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/0e7b8f01bca0/pharmaceutics-16-01055-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/16a5c9cc19e7/pharmaceutics-16-01055-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/00f468761ebb/pharmaceutics-16-01055-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/6798360ce50b/pharmaceutics-16-01055-sch001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/5ed362d4200b/pharmaceutics-16-01055-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/d39f09000d65/pharmaceutics-16-01055-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/ae705f11e9c0/pharmaceutics-16-01055-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/07b659212456/pharmaceutics-16-01055-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/5dfe40ab92b1/pharmaceutics-16-01055-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/de3fbe1b277f/pharmaceutics-16-01055-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/639b/11359337/65a84fb5096d/pharmaceutics-16-01055-g010.jpg

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