Rapid dissolving microneedle patch integrated with benidipine-loaded nanotransfersomes for transdermal drug delivery: optimization, characterizations, and preclinical bioavailability assessment.

IF 5.5 3区医学 Q1 MEDICINE, RESEARCH & EXPERIMENTAL

Drug Delivery and Translational Research Pub Date : 2026-05-01 Epub Date: 2025-10-15 DOI:10.1007/s13346-025-01976-9

Khater Al-Japairai, Samah Hamed Almurisi, Fawaz Alheibshy, Nadiya Abdul-Halim, Syed Mahmood

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Abstract

Benidipine hydrochloride (BEN) is widely prescribed for managing hypertension; however, its clinical efficacy is limited by poor oral bioavailability. This study introduces an innovative delivery approach, incorporating BEN-loaded nanotransfersomes (BEN-TF) into a rapid dissolving microneedles (DMNs) patch for transdermal administration. The nanotransfersomal formulation was optimised via a Box-Behnken design following preparation using a thin-film hydration method. The optimised formulation exhibited favourable characteristics, including a vesicle size of 124.9 ± 1.49 nm, high entrapment efficiency (98.12 ± 0.18%), and transdermal flux of 9.74 ± 0.53 μg/cm²/hr. DSC, ATR-FTIR, and XRD analyses confirmed the amorphous state of BEN. Imaging via FESEM and HRTEM demonstrated spherical, uniform nanosized vesicles. Confocal microscopy revealed deep skin penetration. The integration of BEN-TF into DMNs (BEN-TF-DMNs) resulted in efficient skin insertion, rapid dissolution, and good mechanical strength. Ex-vivo results indicated superior permeation compared to BEN-TF or BEN-DMNs alone, while the in-vivo study confirmed improved bioavailability versus both oral tablets and BEN-DMNs. This hybrid delivery platform offers a promising strategy for improving the systemic delivery of BEN.

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快速溶解微针贴片整合负载苯尼地平的纳米转移体用于透皮给药：优化，表征和临床前生物利用度评估。

盐酸苯地平（BEN）被广泛用于治疗高血压；但口服生物利用度差，限制了其临床疗效。本研究介绍了一种创新的给药方法，将负载ben的纳米转移体（BEN-TF）结合到快速溶解的微针（DMNs）贴片中进行透皮给药。采用薄膜水化法制备后，通过Box-Behnken设计优化纳米转移体配方。优化后的配方囊泡大小为124.9±1.49 nm，包封效率为98.12±0.18%，透皮通量为9.74±0.53 μg/cm2/hr。DSC、ATR-FTIR和XRD分析证实了BEN的非晶态。FESEM和HRTEM成像显示球形、均匀的纳米级囊泡。共聚焦显微镜显示深皮肤穿透。将BEN-TF整合到DMNs （BEN-TF-DMNs）中，具有有效的植皮、快速溶解和良好的机械强度。离体结果表明，与单独使用BEN-TF或BEN-DMNs相比，其渗透性更好，而体内研究证实，与口服片剂和BEN-DMNs相比，生物利用度更高。这种混合交付平台为改进BEN的系统交付提供了一种有希望的策略。

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来源期刊

Drug Delivery and Translational Research MEDICINE, RESEARCH & EXPERIMENTALPHARMACOL-PHARMACOLOGY & PHARMACY

CiteScore

11.70

自引率

1.90%

发文量

160

期刊介绍： The journal provides a unique forum for scientific publication of high-quality research that is exclusively focused on translational aspects of drug delivery. Rationally developed, effective delivery systems can potentially affect clinical outcome in different disease conditions. Research focused on the following areas of translational drug delivery research will be considered for publication in the journal. Designing and developing novel drug delivery systems, with a focus on their application to disease conditions; Preclinical and clinical data related to drug delivery systems; Drug distribution, pharmacokinetics, clearance, with drug delivery systems as compared to traditional dosing to demonstrate beneficial outcomes Short-term and long-term biocompatibility of drug delivery systems, host response; Biomaterials with growth factors for stem-cell differentiation in regenerative medicine and tissue engineering; Image-guided drug therapy, Nanomedicine; Devices for drug delivery and drug/device combination products. In addition to original full-length papers, communications, and reviews, the journal includes editorials, reports of future meetings, research highlights, and announcements pertaining to the activities of the Controlled Release Society.