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脱水山梨醇单硬脂酸酯如何提高脂质核聚合物纳米胶囊的载药量。

How Sorbitan Monostearate Can Increase Drug-Loading Capacity of Lipid-Core Polymeric Nanocapsules.

作者信息

Poletto Fernanda S, De Oliveira Catiúscia P, Wender Heberton, Regent Dorothée, Donida Bruna, Teixeira Sérgio R, Guterres Sílvia S, Rossi-Bergmann Bartira, Pohlmann Adriana R

出版信息

J Nanosci Nanotechnol. 2015 Jan;15(1):827-37. doi: 10.1166/jnn.2015.9182.

Abstract

Lipid-core polymeric nanocapsules are innovative devices that present distinguished characteristics due to the presence of sorbitan monostearate into the oily-core. This component acted as low-molecular-mass organic gelator for the oil (medium chain triglycerides). The organogel-structured core influenced the polymeric wall characteristics disfavoring the formation of more stable polymer crystallites. This probably occurred due to interpenetration of these pseudo-phases. Sorbitan monostearate dispersed in the oily-core was also able to interact by non-covalent bonding with the drugs increasing the drug loading capacity more than 40 times compared to conventional nanocapsules. We demonstrated that the drug-models quercetin and quercetin pentaacetate stabilized the organogel network probably due to interactions of the drug molecules with the sorbitan monostearate headgroups by hydrogen bonding.

摘要

脂质核聚合物纳米胶囊是一种创新型制剂,由于在油相中存在单硬脂酸山梨坦,因而具有显著特性。该成分作为油(中链甘油三酯)的低分子量有机胶凝剂。有机凝胶结构的核影响了聚合物壁的特性,不利于形成更稳定的聚合物微晶。这可能是由于这些假相的相互渗透所致。分散在油相中的单硬脂酸山梨坦还能够通过非共价键与药物相互作用,与传统纳米胶囊相比,药物负载能力提高了40多倍。我们证明,药物模型槲皮素和槲皮素五乙酸酯可能由于药物分子与单硬脂酸山梨坦头基通过氢键相互作用而稳定了有机凝胶网络。

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