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Topical Cream-Based Dosage Forms of the Macrocyclic Drug Delivery Vehicle Cucurbit6uril

机译:大环药物递送载体葫芦6 uril的局部乳膏剂型

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摘要

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. Atudconcentrations 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.
机译:称为葫芦[ur]的分子的大环家族是潜在的药物传递载体,因为它们能够与许多不同种类的药物形成宿主-客体复合物。这项研究旨在检查葫芦[6]尿素(CB [6])在局部乳膏剂中用于局部治疗或经皮递送的效用。将葫芦[6]尿素配制成缓冲性乳膏水基和油性乳膏剂型。通过差示扫描量热法研究了CB [6]与其他赋形剂的固态相互作用,并使用大鼠皮肤测定了大环化合物的透皮渗透性。在CB [6]和其他剂型赋形剂之间观察到了显着的固态相互作用。浓度高达32%w / w时,缓冲的水性乳膏可以保持其正常稠度,可以有效地应用于皮肤,但是油性乳膏太硬,不适合用作剂型。葫芦[6]尿素不渗透皮肤。因此,结果暗示基于葫芦素的外用乳膏可能仅可用于局部皮肤治疗,而不能用于透皮给药。

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