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基于大环药物传递载体葫芦脲的乳膏剂型。

Topical cream-based dosage forms of the macrocyclic drug delivery vehicle cucurbit[6]uril.

机构信息

Faculty of Pharmacy, The University of Sydney, Sydney, New South Whales, Australia.

出版信息

PLoS One. 2014 Jan 15;9(1):e85361. doi: 10.1371/journal.pone.0085361. eCollection 2014.

Abstract

The macrocycle family of molecules called cucurbit[n]urils are potential drug delivery vehicles as they are able to form host-guest complexes with many different classes of drugs. This study aimed to examine the utility of Cucurbit[6]uril (CB[6]) in topical cream-based formulations for either localised treatment or for transdermal delivery. Cucurbit[6]uril was formulated into both buffered cream aqueous- and oily cream-based dosage forms. The solid state interaction of CB[6] with other excipients was studied by differential scanning calorimetry and the macrocycle's transdermal permeability was determined using rat skin. Significant solid state interactions were observed between CB[6] and the other dosage form excipients. At concentrations up to 32% w/w the buffered aqueous cream maintained its normal consistency and could be effectively applied to skin, but the oily cream was too stiff and is not suitable as a dosage form. Cucurbit[6]uril does not permeate through skin; as such, the results imply that cucurbituril-based topical creams may potentially only have applications for localised skin treatment and not for transdermal drug delivery.

摘要

大环分子家族称为葫芦[n]脲是潜在的药物输送载体,因为它们能够与许多不同类别的药物形成主客体配合物。本研究旨在考察葫芦[6]脲(CB[6])在局部治疗或经皮给药的乳膏基制剂中的应用。将葫芦[6]脲分别配制在缓冲乳膏水相和油性乳膏基制剂中。通过差示扫描量热法研究 CB[6]与其他赋形剂的固态相互作用,并使用大鼠皮肤测定大环的经皮渗透性。观察到 CB[6]与其他制剂辅料之间存在显著的固态相互作用。在高达 32%w/w 的浓度下,缓冲水性乳膏保持其正常稠度,并可有效地施用于皮肤,但油性乳膏太硬,不适合作为制剂。葫芦[6]脲不能透过皮肤;因此,结果表明基于葫芦脲的局部用乳膏可能仅适用于局部皮肤治疗,而不适用于经皮药物递送。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/ac43/3893214/30f3f3c14ff8/pone.0085361.g001.jpg

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