In-Vivo Investigation of the Irritation potential of Lamivudine and Stavudine liposomal gels in rabbits

R. Pai, D. Kusum, D. Kshama, S. Fattepur
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Abstract

Effective antiretroviral therapy is required on a long-term basis to maintain viral suppression and reduce disease progression in HIV infections. An attempt has been made to implement the principles of novel drug delivery to antiretrovirals in order to overcome the drawbacks of existing therapy. Liposomal gels of lamivudine and stavudine respectively were developed for the transdermal drug delivery. The irritation potential of drug loaded and blank formulations was investigated on shaved rabbit skin, in vivo, and compared to that of 5% sodium lauryl sulphate (SLS) solution (a known irritant) as the positive control and untreated portion of the skin as a negative control. Skin irritation was assessed by visual observations and histological evaluations. We found that the drug loaded and blank liposomal gels caused no significant epidermal irritation and erythema. Thus we conclude that these liposomal gels may be used safely as transdermal drug delivery vehicles for the selected antiretrovirals.
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拉米夫定和司他夫定脂质体凝胶在家兔体内刺激电位的研究
需要长期有效的抗逆转录病毒治疗,以维持病毒抑制和减少艾滋病毒感染的疾病进展。为了克服现有治疗方法的缺点,已经尝试实施抗逆转录病毒药物递送的新原理。制备了拉米夫定和司他夫定经皮给药的脂质体凝胶。研究了载药和空白制剂对兔剃毛皮肤的体内刺激电位,并与5%十二烷基硫酸钠(SLS)溶液(一种已知刺激物)作为阳性对照和未处理部分皮肤作为阴性对照进行了比较。通过视觉观察和组织学评估皮肤刺激程度。我们发现载药和空白脂质体凝胶没有引起明显的表皮刺激和红斑。因此,我们得出结论,这些脂质体凝胶可以安全地用作经皮给药载体,用于选定的抗逆转录病毒药物。
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