QBD based Design and Characterization of Proniosomal Transdermal Delivery of Atenolol and Glibenclamide Combination: An Innovative Approach

P. Anitha, S. Ramkanth, S. Satyanarayana
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引用次数: 2

Abstract

There are numerous circumstances where chronic disease is associated with other disorders, especially in diseases like diabetes with noncommunicable disease risk factors, such as hypertension. This study shows a novel and innovative combinational proniosomal delivery of combination to beat the reactions by complex therapeutic regimen, and to improve patient compliance after controlling combinational transdermal delivery of Glibenclamide (GLB) and Atenolol (ATN) which have not been tried actually. To achieve the above reason, proniosomes were prepared and optimized utilizing Box-Behnken design. The ideal formulation was chosen by a point prediction method and formulation showed vesicle size of 562 ± 1.223 nm, entrapment efficiency of GLB & ATN 97.037 ± 1.43% and 96.230 ± 1.62% respectively which were found in concurrence with the predicted value. The optimized combinational proniosomal gel (OCPG) formulation was additionally assessed for in vitro drug release, In vitro drug permeation, and in vivo pharmacokinetic study. The OCPG formulation shows the greatest flux over the rabbit skin (128.609 ± 2.24 mg/cm/h and 322.054 ± 1.53 mg/ cm/h) of GLB and ATN respectively. The results indicated desired release and permeation profiles. OCPG showed significantly (p < 0.001) pharmacokinetic contemplate exhibited that transdermal proniosomal formulation demonstrated improvement in bioavailability of two drugs 129.30 and 174.62 times respectively as that of the oral formulation. Overall the results show that controlled release GLB and ATN provesicles offer a useful and promising transdermal delivery system for the treatment of type II diabetes and hypertension by using design. Henceforth this may be an achievement in treating diabetic hypertensive patient.
基于QBD的阿替洛尔和格列本脲联合前体经皮给药设计和表征:一种创新方法
在许多情况下,慢性病与其他疾病有关,特别是糖尿病等具有高血压等非传染性疾病风险因素的疾病。本研究提出了一种新颖创新的前体联合给药方案,以克服复杂治疗方案的反应,并在控制格列本脲(GLB)和阿替洛尔(ATN)联合经皮给药后,提高患者的依从性。为达到上述目的,利用Box-Behnken设计对原体进行制备和优化。采用点预测法优选出理想配方,其囊泡大小为562±1.223 nm, GLB和ATN的包封效率分别为97.037±1.43%和96.230±1.62%,与预测值一致。并对优化后的复方前质体凝胶(OCPG)进行了体外释药、体外渗透和体内药代动力学研究。OCPG制剂在兔皮肤上的GLB和ATN通量最大(分别为128.609±2.24 mg/cm/h和322.054±1.53 mg/cm/h)。结果显示了理想的释放和渗透曲线。OCPG显示显著(p < 0.001)药代动力学观察显示经皮前体制剂比口服制剂分别提高了129.30倍和174.62倍的生物利用度。综上所述,GLB和ATN控释微胶囊通过设计为治疗II型糖尿病和高血压提供了一种有用的、有前途的透皮给药系统。因此,这可能是治疗糖尿病高血压患者的一项成果。
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