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采用质量源于设计理念开发载比马前列素脂质纳米制剂:用于降低眼压的脂质体与固体脂质纳米粒比较

Bimatoprost-loaded lipidic nanoformulation development using quality by design: liposomes versus solid lipid nanoparticles in intraocular pressure reduction.

作者信息

Verma Piyush, Singh Rishi Kumar, Wadhwa Anubhav, Prabhakar Bala, Yadav Khushwant S

机构信息

Shobhaben Pratapbhai Patel School of Pharmacy & Technology Management, SVKM's NMIMS (Deemed to be University), Mumbai, 400056, India.

出版信息

Nanomedicine (Lond). 2023 Nov 22. doi: 10.2217/nnm-2023-0141.

Abstract

Bimatoprost is a drug used to lower intraocular pressure in the treatment of glaucoma. Conventional eye drops have the limitations of repeated dosing, drug loss due to tear outflow and hence poor availability for action. Using a systematic quality by design approach, liposomes and solid lipid nanoparticles were formulated and further encapsulated in thermo-sensitive hydrogel. Optimized liposomes had 87.04% encapsulation efficiency and 306.78 nm mean particle size, while solid lipid nanoparticles had 90.51% and 304.21 nm. Bimatoprost liposomes had controlled zero-order drug kinetics and no initial burst release, making them better than solid lipid nanoparticles. Bimatoprost-loaded liposomes in thermo-sensitive hydrogel decreased intraocular pressure for 18 h.

摘要

比马前列素是一种用于治疗青光眼以降低眼压的药物。传统眼药水存在重复给药的局限性,会因泪液流出导致药物流失,因此药物起效的可用性较差。采用系统的质量源于设计方法,制备了脂质体和固体脂质纳米粒,并进一步将其包封在热敏水凝胶中。优化后的脂质体包封率为87.04%,平均粒径为306.78 nm,而固体脂质纳米粒的包封率为90.51%,平均粒径为304.21 nm。比马前列素脂质体具有可控的零级药物动力学且无初始突释现象,使其优于固体脂质纳米粒。负载比马前列素的热敏水凝胶脂质体可降低眼压达18小时。

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