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用于改善难溶性药物递送的胶囊型脂质口服制剂。

Lipid-based oral formulation in capsules to improve the delivery of poorly water-soluble drugs.

作者信息

Mohite Popat, Singh Sudarshan, Pawar Anil, Sangale Adinath, Prajapati Bhupendra G

机构信息

A.E.T.s St. John Institute of Pharmacy and Research, Palghar, Maharashtra, India.

Department of Pharmaceutical Sciences, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.

出版信息

Front Drug Deliv. 2023 Aug 24;3:1232012. doi: 10.3389/fddev.2023.1232012. eCollection 2023.

Abstract

Poorly water-soluble drugs demonstrate significant challenge in pharmaceutical development, which is linked to their limited oral bioavailability and therapeutic efficacy. To overcome these limitations, lipid-based formulations have emerged as a promising approach to enhance the delivery of such drugs. Moreover, encapsulation within capsules to provide a convenient dosage form for oral administration. The encapsulation techniques are optimized to ensure uniform drug content and efficient encapsulation efficiency. Several investigations demonstrated that the lipid-based formulations in capsules significantly improved the solubility and dissolution rate of poorly water-soluble drugs compared to non-lipid formulations. Additionally, the encapsulation of lipid-based formulations protected the drug against degradation and improved its stability. Overall, incorporating lipid-based formulations in capsules represents a promising strategy for enhancing the delivery of poorly water-soluble drugs with improvement in solubility, dissolution, stability, and bioavailability, overcoming the challenges associated with these challenging drug molecules. The review focussed a brief on utilization of lipids in capsule form to improve therapeutic efficacy of poorly soluble, dissolution and bioavailability of drugs.

摘要

水溶性差的药物在药物研发中面临重大挑战,这与其有限的口服生物利用度和治疗效果有关。为克服这些限制,基于脂质的制剂已成为增强此类药物递送的一种有前景的方法。此外,将其封装在胶囊中以提供方便的口服剂型。对封装技术进行了优化,以确保药物含量均匀且封装效率高。多项研究表明,与非脂质制剂相比,胶囊中的基于脂质的制剂显著提高了水溶性差的药物的溶解度和溶解速率。此外,基于脂质的制剂的封装保护了药物不被降解并提高了其稳定性。总体而言,将基于脂质的制剂纳入胶囊是一种有前景的策略,可增强水溶性差的药物的递送,改善其溶解度、溶解、稳定性和生物利用度,克服与这些具有挑战性的药物分子相关的挑战。该综述简要聚焦了以胶囊形式使用脂质来提高难溶性药物的治疗效果、溶解度和生物利用度。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/02d0/12363274/0ea8bdc66912/fddev-03-1232012-g001.jpg

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