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首页> 外文期刊>Drug Design, Development and Therapy >Solubilization of beclomethasone dipropionate in sterically stabilized phospholipid nanomicelles (SSMs): physicochemical and in vitro evaluations
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Solubilization of beclomethasone dipropionate in sterically stabilized phospholipid nanomicelles (SSMs): physicochemical and in vitro evaluations

机译：倍氯米松双丙酸酯在空间稳定的磷脂纳米胶束（SSMs）中的增溶：理化和体外评价

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Background: The local treatment of lung disorders such as asthma and chronic obstructive pulmonary disease via pulmonary drug delivery offers many advantages over oral or intravenous routes of administration. This is because direct deposition of a drug at the diseased site increases local drug concentrations, which improves the pulmonary receptor occupancy and reduces the overall dose required, therefore reducing the side effects that result from high drug doses. From a clinical point of view, although jet nebulizers have been used for aerosol delivery of water-soluble compounds and micronized suspensions, their use with hydrophobic drugs has been inadequate.Aim: To evaluate the feasibility of sterically stabilized phospholipid nanomicelles (SSMs) loaded with beclomethasone dipropionate (BDP) as a carrier for pulmonary delivery.Methods: 1,2-Distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 5000) polymeric micelles containing BDP (BDP-SSMs) were prepared by the coprecipitation and reconstitution method, and the physicochemical and in vitro characteristics of BDP-SSMs were investigated.Results: BDP-SSMs were successfully prepared with a content uniformity and reproducibility suitable for pulmonary administration. The maximum solubility of BDP in SSMs was approximately 1300 times its actual solubility. The particle size and zeta potential of BDP-SSMs were 19.89 ± 0.67 nm and -28.03 ± 2.05 mV, respectively. The SSMs system slowed down the release of BDP and all of the aerodynamic values of the aerosolized rehydrated BDP-SSMs were not only acceptable but indicated a significant level of deposition in the lungs.Conclusion: The SSM system might be an effective way of improving the therapeutic index of nebulized, poorly soluble corticosteroids.
机译：背景：通过肺部药物递送对肺部疾病（如哮喘和慢性阻塞性肺疾病）进行局部治疗与口服或静脉内给药途径相比具有许多优势。这是因为将药物直接沉积在患病部位会增加局部药物浓度，从而改善了肺部受体的占有率并降低了所需的总剂量，因此减少了因高剂量药物引起的副作用。从临床角度来看，尽管喷射雾化器已用于水溶性化合物和微粉化悬浮液的气雾剂输送，但它们与疏水性药物的使用仍不充分。方法：以1,2,2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺-N-甲氧基-聚乙二醇（BDP-SSMs）为原料制备1,2-二硬脂酰基-sn-甘油-3-磷酸乙醇胺-N-甲氧基-聚（乙二醇5000）聚合物胶束。结果：成功制备了BDP-SSMs，其含量均匀性和重现性好，适用于肺部给药。通过对BDP-SSMs的共沉淀和重构方法进行了研究。 BDP在SSM中的最大溶解度约为其实际溶解度的1300倍。 BDP-SSM的粒径和Zeta电位分别为19.89±0.67 nm和-28.03±2.05 mV。 SSMs系统减慢了BDP的释放速度，雾化的再水化BDP-SSMs的所有空气动力学值不仅可以接受，而且表明其在肺中的沉积水平很高。结论：SSM系统可能是改善BDP的有效方法。雾化的难溶性皮质类固醇激素的治疗​​指数。

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