Nanoemulsion-laden poly(vinyl) alcohol hydrogel films for transdermal delivery of carbamazepine

IF 3.8 4区工程技术 Q2 CHEMISTRY, APPLIED

Journal of Vinyl & Additive Technology Pub Date : 2024-05-13 DOI:10.1002/vnl.22116

Manali Rai, Preeti Lakra, Harsh Yadav, Sabyasachi Maiti

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Abstract

There is an unmet demand for transdermal devices that can deliver large dose of medications through the skin. Herein, nanoemulsion-based poly(vinyl alcohol) (PVA) transdermal hydrogel films were developed for the high-dose anti-epileptic drug carbamazepine. A stable nanoemulsion was created with almond oil, Tween 60, and amphiphilic locust bean gum. The nanoemulsion had a hydrodynamic diameter of 251 nm, a polydispersity of 10.3%, and a zeta potential of −51.2 mV. Carbamazepine-loaded nanoemulsion was blended with carbamazepine-free PVA dispersion and casted into films. To accommodate a high dose, carbamazepine-loaded nanoemulsion was trapped in a PVA dispersion containing carbamazepine to create transdermal films. The physicochemical characteristics and drug penetration characteristics of the produced films were compared. Both films had the uniform thickness, weight, and drug content. The folding endurance was found to be greater than 700 in both cases. Water vapor permeability decreased when carbamazepine was added to almond oil as well as polymer dispersion. FESEM pictures revealed a waxy paper-like appearance for the PVA hydrogel film with dual drug-reservoirs. FTIR spectra assessment revealed a hydrogen bonding interaction between PVA and carbamazepine. X-ray diffraction examination revealed that the film contained an amorphous dispersion of carbamazepine. Dual carbamazepine reservoir-based films outperformed single nanoemulsion drug reservoir-based films in terms of drug flux through excised rat skin by 3.2 times. The in vitro skin permeation findings corresponded well to zero order kinetic models. Overall, this study showed that a high-dose drug could be placed on nanoemulsion-based transdermal PVA hydrogel films, resulting in improved skin permeability.

Highlights

Nanoemulsion was stable at almond oil:Tween 60/modified gum ratio of 5:5.
Loading of high dose carbamazepine in nanoemulsion-PVA transdermal films.
Film of dual carbamazepine reservoir showed low water vapor permeation, moisture retention.
Flux of carbamazepine from films improved three times through excised rat skin.

Abstract Image

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纳米乳液添加聚乙烯醇水凝胶薄膜用于卡马西平的透皮给药

人们对能通过皮肤输送大剂量药物的透皮装置的需求尚未得到满足。在此，我们为大剂量抗癫痫药物卡马西平开发了基于纳米乳液的聚乙烯醇（PVA）透皮水凝胶薄膜。用杏仁油、吐温 60 和两亲性槐豆胶制成了稳定的纳米乳液。纳米乳液的流体力学直径为 251 nm，多分散性为 10.3%，Zeta 电位为 -51.2 mV。含卡马西平的纳米乳液与不含卡马西平的 PVA 分散体混合后浇铸成薄膜。为了适应高剂量，在含有卡马西平的 PVA 分散液中加入了卡马西平纳米乳液，制成透皮膜。比较了所制备薄膜的理化特性和药物渗透特性。两种薄膜的厚度、重量和药物含量均一致。两种薄膜的耐折度均大于 700。在杏仁油和聚合物分散体中添加卡马西平后，水蒸气渗透性降低。FESEM 照片显示，具有双药物储库的 PVA 水凝胶薄膜呈现蜡纸状外观。傅立叶变换红外光谱评估显示，PVA 和卡马西平之间存在氢键相互作用。X 射线衍射检查显示，薄膜中含有无定形分散的卡马西平。就药物通过切除的大鼠皮肤的通量而言，双卡马西平储层薄膜是单一纳米乳液药物储层薄膜的 3.2 倍。体外皮肤渗透结果与零阶动力学模型十分吻合。亮点纳米乳液在杏仁油：吐温 60/改性树胶的比例为 5:5 时是稳定的。在纳米乳液-PVA透皮膜中加入高剂量卡马西平。双卡马西平储藏膜的水蒸气渗透率低，保湿性好。通过切除的大鼠皮肤，薄膜中卡马西平的通量提高了三倍。

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来源期刊

Journal of Vinyl & Additive Technology 工程技术-材料科学：纺织

CiteScore

5.40

自引率

14.80%

发文量

审稿时长

>12 weeks

期刊介绍： Journal of Vinyl and Additive Technology is a peer-reviewed technical publication for new work in the fields of polymer modifiers and additives, vinyl polymers and selected review papers. Over half of all papers in JVAT are based on technology of additives and modifiers for all classes of polymers: thermoset polymers and both condensation and addition thermoplastics. Papers on vinyl technology include PVC additives.