Madhavi Nimmathota, Ganji Naveen Kumar, Battu Heera, Sudhakar Beeravelli
Department of Pharmaceutics, CMR College of Pharmacy, Medchal, Kandlakoya, Hyderabad, Telangana 501401, India.
Department of Pharmaceutics, Brown's College of Pharmacy, Affiliated to Kakatiya University, Ammapalem, Khammam, Telangana 507305, India.
Nanotheranostics. 2025 May 7;9(2):144-154. doi: 10.7150/ntno.110819. eCollection 2025.
The present study aimed to overcome the drawbacks of tapentadol through the oral route and to assess the significance of microemulsion gels for transdermal delivery via pharmacokinetic approach. Microemulsions were prepared via a ternary phase diagram. The optimized microemulsion was converted into gels, and the microemulsion was evaluated for particle size, zeta potential and cumulative drug release, whereas the gel was characterized for viscosity, spreadability, , , and skin irritation studies. The prepared ME-gel PKs were tested against MEs, oral solution and plain gel. The PK study revealed that the half-life of the ME gel was 2.2-fold greater than that of the oral solution and 1.65-fold greater than that of the plain gel. The MRT of the ME gel was 6-fold greater than that of the oral solution and 3.3-fold greater than that of the plain gel. The overall mean value of the AUC (0-∞) was 3.16 times greater than that of the oral route. The skin irritation studies found that absence of irritation and damage after application of ME-gel. The PK study revealed that ME-gel was effective in pain management. The level A IVIVC between the fraction of drug released and the fraction of drug absorbed was 0.9731.
本研究旨在克服他喷他多口服给药途径的缺点，并通过药代动力学方法评估微乳凝胶经皮给药的意义。通过三元相图制备微乳。将优化后的微乳转化为凝胶，并对微乳的粒径、zeta电位和药物累积释放进行评估，而对凝胶的粘度、铺展性、……和皮肤刺激性进行研究。将制备的微乳凝胶的药代动力学与微乳、口服溶液和普通凝胶进行对比测试。药代动力学研究表明，微乳凝胶的半衰期比口服溶液长2.2倍，比普通凝胶长1.65倍。微乳凝胶的平均滞留时间比口服溶液长6倍，比普通凝胶长3.3倍。AUC(0-∞)的总体平均值比口服途径高3.16倍。皮肤刺激性研究发现，应用微乳凝胶后无刺激和损伤。药代动力学研究表明，微乳凝胶在疼痛管理方面有效。药物释放分数与药物吸收分数之间的A级体内体外相关性为0.9731。
