UGC-Centre of Excellence in Applications of Nanomaterials, Nanoparticles and Nanocomposites, Panjab University, Chandigarh 160 014, India.
Int J Pharm. 2013 Nov 1;456(1):65-72. doi: 10.1016/j.ijpharm.2013.08.019. Epub 2013 Aug 23.
Tretinoin (TRE) is a widely used retinoid for the topical treatment of acne, psoriasis, skin cancer and photoaging. Despite unmatchable efficacy, it is associated with several vexatious side effects like marked skin erythema, peeling and irritation, eventually leading to poor patient compliance. Its photo-instability and high lipophilicity also pose challenges in the development of a suitable topical product. The present study, therefore, aims to develop biocompatible lipid-based nanocarriers of TRE to improve its skin delivery, photostability, biocompatibility and pharmacodynamic efficacy. The TRE-loaded liposomes, ethosomes, solid lipid nanoparticles (SLNs) and nanostructured lipidic carriers (NLCs) were prepared and characterized for micromeritics, surface charge, percent drug efficiency and morphology. Bioadhesive hydrogels of the developed systems were also evaluated for rheological characterization, photostability, ex vivo skin permeation and retention employing porcine skin, and anti-psoriatic activity in mouse tail model. Nanoparticulate carriers (SLNs, NLCs) offered enhanced photostability, skin transport and anti-psoriatic activity vis-à-vis the vesicular carriers (liposomes, ethosomes) and the marketed product. However, all the developed nanocarriers were found to be more biocompatible and effective than the marketed product. These encouraging findings can guide in proper selection of topical carriers among diversity of such available carriers systems.
维 A 酸（TRE）是一种广泛用于治疗痤疮、银屑病、皮肤癌和光老化的外用维 A 酸类药物。尽管疗效无可比拟，但它也与一些令人烦恼的副作用有关，如明显的皮肤红斑、脱皮和刺激，最终导致患者顺应性差。其光不稳定性和高亲脂性也给合适的局部产品的开发带来了挑战。因此，本研究旨在开发生物相容性的脂质纳米载体来提高其皮肤传递、光稳定性、生物相容性和药效。制备并表征了载 TRE 的脂质体、醇质体、固体脂质纳米粒（SLN）和纳米结构脂质载体（NLC），以评估其微细化、表面电荷、药物效率和形态。还评估了开发系统的生物粘附水凝胶的流变特性、光稳定性、离体皮肤渗透和保留情况，使用猪皮，并在小鼠尾巴模型中评估其抗银屑病活性。与囊泡载体（脂质体、醇质体）和市售产品相比，纳米载体（SLN、NLC）具有更好的光稳定性、皮肤传递和抗银屑病活性。然而，所有开发的纳米载体都比市售产品更具生物相容性和有效性。这些令人鼓舞的发现可以指导在多种现有载体系统中选择合适的局部载体。
