采用改良脂质体凝胶共递送过氧化苯甲酰和阿达帕林用于改善痤疮治疗。
Codelivery of benzoyl peroxide & adapalene using modified liposomal gel for improved acne therapy.
机构信息
Department of Pharmaceutics, National, Centre for Pharmaceutical Nanotechnology, Institute of Pharmaceutical Education & Research (NIPER), Sector 67, S.A.S. Nagar (Mohali) Punjab, 160062, India.
出版信息
Nanomedicine (Lond). 2018 Jun;13(12):1481-1493. doi: 10.2217/nnm-2018-0002. Epub 2018 Jul 4.
AIM
Current study investigates therapeutic efficacy and tolerability of benzoyl peroxide (BPO)- and adapalene (AD)-loaded modified liposomal gel (BPO-AD-mLipo gel) for improved acne therapy.
MATERIALS & METHOD: BPO-AD-mLipo were optimized and loaded in Carbopol gel. Both BPO-AD-mLipo and BPO-AD-mLipo-gel were extensively characterized for different quality attributes. Ex vivo dermal bioavailability, dermal distribution, in vivo anti-acne efficacy and skin irritation studies were performed and compared with marketed formulation (Epiduo, Galderma Laboratories LP, TX, USA).
RESULTS
BPO-AD-mLipo illustrated size 256.4 ± 9.3 nm with polydispersity index ∼ 0.2. Significantly enhanced dermal bioavailability (AD-2.1, 5.4; BPO-3.0, 7.83-fold) and reduction in skin irritation and papule density in animal model were observed with BPO-AD-mLipo-gel as compared with free drugs and Epiduo, respectively.
CONCLUSION
BPO-AD-mLipo gel provides effective and safer alternative approach for codelivery of anti-acne drugs.
目的
本研究旨在考察载过氧化苯甲酰（BPO）和阿达帕林（AD）的改良脂质体凝胶（BPO-AD-mLipo 凝胶）的治疗效果和耐受性，以改善痤疮治疗效果。
材料与方法
对 BPO-AD-mLipo 进行优化并载入卡波姆凝胶中。对 BPO-AD-mLipo 和 BPO-AD-mLipo-凝胶进行了广泛的质量属性表征。并进行了体外皮肤生物利用度、皮肤分布、体内抗痤疮功效和皮肤刺激性研究，并与市售制剂（Epiduo，Galderma Laboratories LP，TX，USA）进行了比较。
结果
BPO-AD-mLipo 的粒径为 256.4±9.3nm，多分散指数约为 0.2。与游离药物和 Epiduo 相比，BPO-AD-mLipo-凝胶显著提高了 AD 的皮肤生物利用度（增加 2.1、5.4 倍），降低了皮肤刺激性和丘疹密度。
结论
BPO-AD-mLipo 凝胶为载药治疗痤疮提供了一种更有效、更安全的方法。
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