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首页> 外文期刊>Journal of Microencapsulation: Microcapsules Liposomes Nanoparticles Microcells Microspheres >SLN and NLC for topical delivery of ketoconazole
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SLN and NLC for topical delivery of ketoconazole

机译：SLN和NLC用于酮康唑的局部给药

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摘要

The clinical use of ketoconazole has been related to some adverse effects in healthy adults,specially local reactions,such as severe irritation,pruritus and stinging.The purpose of the present work is the assessment of ketoconazole stability in aqueous SLN and NLC dispersions,as well as the phy-sicochemical stability of these lipid nanoparticles,which might be useful for targeting this drug into topical route,minimizing the adverse side effects and providing a controlled release.Lipid particles were prepared using Compritol~R 888 ATO as solid lipid.The natural antioxidant a-tocopherol was selected as liquid lipid compound for the preparation of NLC.Ketoconazole loading capacity was identical for both SLN and NLC systems (5% of particle mass).SLN were physically stable as suspensions during 3 months of storage,but the SLN matrix was not able to protect the chemically labile ketoconazole against degradation under light exposure.In contrast,the NLC were able to stabilize the drug,but the aqueous NLC dispersion showed size increase during storage.Potential topical formulations are light-protected packaged SLN or NLC physically stabilized in a gel formulation.
机译：酮康唑的临床使用已与健康成年人的某些不良反应，特别是局部反应有关，例如严重的刺激性，瘙痒和刺痛。本研究的目的是评估酮康唑在SLN和NLC水性分散液中的稳定性。作为这些脂质纳米颗粒的物理化学化学稳定性，可能有助于将该药物靶向局部途径，减少不良副作用并提供控释作用。使用Compritol〜R 888 ATO作为固体脂质制备脂质颗粒。抗氧化剂α-生育酚被选作制备NLC的液体脂质化合物。酮康唑在SLN和NLC系统中的负载量相同（占颗粒质量的5％）。SLN在悬浮液中3个月的物理稳定性稳定，但SLN基质不能保护化学不稳定的酮康唑在光照下不会降解。相反，NLC能够稳定药物，但是NLC水性分散液在储存过程中显示尺寸增加。潜在的局部用制剂为避光包装的SLN或NLC，在凝胶制剂中物理稳定。

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