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基于聚乳酸-羟基乙酸共聚物的热熔挤出整体丝材:体外比较研究。

PLGA-based monolithic filaments prepared by hot-melt extrusion: In-vitro comparative study.

作者信息

Kamel R, Abbas H

机构信息

Pharmaceutical Technology Department, National Research Center, El-Bohooth street, Cairo, Egypt.

Pharmaceutics department, Damanhour University, Egypt.

出版信息

Ann Pharm Fr. 2018 Mar;76(2):97-106. doi: 10.1016/j.pharma.2017.09.002. Epub 2017 Nov 14.

Abstract

To avoid frequent drug administration, PLGA-based monolithic filament-shaped implants were prepared. In this study, the effect of different formulation variables was studied, namely: type of PLGA (PLGA 502 and PLGA 503), type of drug (the lipophilic Prednisolone acetate, PA and the hydrophilic Propranolol Hydrochloride, PH) and drug loading (10 and 30% w/w). PLGA 503-based implants showed a lower water uptake, lower mass loss and erosion, slower drug release, and better mechanical properties and elasticity (P<0.05) compared to the corresponding PLGA 502-based implants. PH-loaded implants showed a faster swelling and degradation as well as drug release (P<0.05) compared to PA-loaded implants; the former attained almost complete drug release after about 18 days, while the latter attained it after about 30 days. All the implants followed a zero-order kinetic pattern suitable for a controlled drug release. Characterization was done using SEM and DSC. This study proved the potential tailoring of the properties of PLGA-implants, prepared by hot-melt extrusion (HME), based on some formulation variables.

摘要

为避免频繁给药,制备了基于聚乳酸-羟基乙酸共聚物(PLGA)的整体丝状植入物。在本研究中,研究了不同配方变量的影响,即:PLGA的类型(PLGA 502和PLGA 503)、药物类型(亲脂性的醋酸泼尼松龙,PA和亲水性的盐酸普萘洛尔,PH)和药物载量(10%和30%w/w)。与相应的基于PLGA 502的植入物相比,基于PLGA 503的植入物表现出更低的吸水率、更低的质量损失和侵蚀、更慢的药物释放以及更好的机械性能和弹性(P<0.05)。与载PA的植入物相比,载PH的植入物表现出更快的溶胀、降解以及药物释放(P<0.05);前者在约18天后几乎达到完全药物释放,而后者在约30天后达到完全药物释放。所有植入物均遵循适合控释的零级动力学模式。使用扫描电子显微镜(SEM)和差示扫描量热法(DSC)进行了表征。本研究证明了基于一些配方变量,通过热熔挤出(HME)制备的PLGA植入物的性能具有潜在的可定制性。

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