Department of Pharmacology, SVKM's Dr. Bhanuben Nanavati College of Pharmacy, Mumbai, India.
Shobhaben Pratapbhai Patel School of Pharmacy and Technology Management, SVKM's NMIMS, Mumbai, India.
J Microencapsul. 2020 Dec;37(8):557-565. doi: 10.1080/02652048.2020.1823499. Epub 2020 Sep 24.
This study was aimed to develop Isotretinoin (ITN) and α-tocopherol acetate (α-TA) loaded solid lipid nanoparticle topical gel for better skin sensitivity and potentiation of efficacy.
ITN and α-TA-loaded solid lipid nanoparticles (AE-SLN) were prepared by microemulsion method with glyceryl mono-stearate as lipid and tween 80: butanol as surfactant and characterised. AE-SLN gel was evaluated for physicochemical characteristics, drug release, skin irritation and anti-acne activity in rats.
AE-SLNs had mean particle size of 193.4 nm (zeta-potential -29 mV) and entrapment efficiency of 84%w/w for ITN and 77.4%w/w for α-TA. AE-SLN gel showed sustained drug release for 24 h with a final cumulative release of 95.8% w/w and 89.1%w/w for ITN and α-TA. AE-SLN gel showed no erythema or edoema in rabbits and potent efficacy in rat model of acne.
In conclusion, AE-SLN gel has the potential to use as a non-irritant topical formulation for the treatment of acne.
本研究旨在开发异维 A 酸（ITN）和醋酸生育酚（α-TA）负载的固体脂质纳米粒 topical 凝胶，以提高皮肤敏感性并增强疗效。
采用微乳法，以单硬脂酸甘油酯为脂质，吐温 80：丁醇为表面活性剂，制备 ITN 和 α-TA 负载的固体脂质纳米粒（AE-SLN），并对其进行了表征。对 AE-SLN 凝胶的理化性质、药物释放、皮肤刺激性和抗痤疮活性进行了评价。
AE-SLNs 的平均粒径为 193.4nm（zeta 电位-29mV），ITN 和 α-TA 的包封效率分别为 84%w/w 和 77.4%w/w。AE-SLN 凝胶在 24 小时内呈现持续药物释放，最终累积释放率分别为 95.8%w/w 和 89.1%w/w。AE-SLN 凝胶在兔体内无红斑或水肿，在痤疮大鼠模型中具有显著疗效。
综上所述，AE-SLN 凝胶具有作为非刺激性 topical 制剂治疗痤疮的潜力。
