Mehta S K, Jindal Neha
Department of Chemistry and Center of Advanced Studies in Chemistry, Panjab University, Chandigarh, 160 014, India,
AAPS PharmSciTech. 2015 Feb;16(1):67-75. doi: 10.1208/s12249-014-0183-y. Epub 2014 Sep 3.
With the aim of assuring more patient compliant pharmacotherapy for acquired immuno deficiency syndrome, a formulation of the first line anti-retroviral drug, nevirapine (NVP), has been developed by encapsulating it within niosomes. Biocompatible niosomes were fabricated using a biological surfactant, tyloxapol, with variable cholesterol concentrations. Formulation with surfactant/cholesterol molar ratio 1:0.1 exhibits maximum stability and optimum hydrophobicity. Thus, it is most suitable for the entrapment of NVP and has high entrapment efficiency of 94.3%. FTIR and DSC results indicate that NVP has sufficient compatibility with the excipients of the formulation. Photoluminescence quenching measurements were employed to elucidate the position of drug molecules in niosome bilayer along with the partition coefficient. Dissolution results indicate that the efflux of drug is sustained which creates a depot effect and decreases the fluctuations in drug release. Such a versatile and improved formulation of NVP is expected to increase its therapeutic index and alleviate toxic systemic side effects while improving the quality of life and duration of survival of the patients.
为确保获得性免疫缺陷综合征患者的药物治疗更具依从性,通过将一线抗逆转录病毒药物奈韦拉平(NVP)包裹于非离子表面活性剂泡囊中来开发其制剂。使用生物表面活性剂泰洛沙泊和不同胆固醇浓度制备生物相容性非离子表面活性剂泡囊。表面活性剂/胆固醇摩尔比为1:0.1的制剂表现出最大稳定性和最佳疏水性。因此,它最适合包封NVP,包封效率高达94.3%。傅里叶变换红外光谱(FTIR)和差示扫描量热法(DSC)结果表明NVP与制剂辅料具有充分的相容性。采用光致发光猝灭测量来阐明药物分子在非离子表面活性剂泡囊双层中的位置以及分配系数。溶出结果表明药物的流出是持续的,这产生了储库效应并减少了药物释放的波动。预计这种多功能且改良的NVP制剂将提高其治疗指数,减轻全身毒性副作用,同时改善患者的生活质量和生存时长。