Formulation and evaluation of nanosized aripiprazole-loaded bionanogels using novel bio-retardant from bark of Cinnamomum verum J.Presl

N. Madhav, Y. Tyagi
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Abstract

The current research work aimed to formulate and evaluate the aripiprazole bionanogel using Cinnamomum verum J.Presl Syn. C. zeylanicum (Lauraceae) as bio-retardant and bio-stabilizer for transcranial delivery. Aripiprazole, a partial dopamine agonist is an antipsychotic drug used in the treatment of schizophrenia, bipolar disorder, major depressive disorder, and irritability associated with autism. The biopolymer from C. verum was isolated by addition of an optimised quantity of acetone and used as bio-retardant and bio-stabilizer to prepare aripiprazole-loaded bionanogels. The initially aripiprazole nanoparticles were prepared by addition of dextrose and dextran as a nanosized agent and various proportion of bio-polymer C. verum as bio-retardant (0.4%, 0.6%, 0.8% and 1%) and guargum (1.5% and 2%) followed by optimised cycles of sonication. The nanoparticles were incorporated uniformly into the gel under magnetic stirrer mode which was prepared by sodium alginate (100 mg), PVA (100 mg) and HPMC (100 mg) and prepared bionanogel was found as the best formulation based on comparison of mentioned parameters i.e. pH, texture, spreadability, % entrapment efficacy, preliminary determination of nano size distribution and in-vitro drug release study. FC3 (1:0.8) containing a retardant showed uniform spreadability, smooth texture and T50% of 51 h and T80% of 72 h, respectively. These formulations can be used for transcranial drug delivery to target the molecule to the brain through the layers of skin, meninges, trigeminal nerves, emissary veins, cranial bones and sutures.
肉桂树皮新型生物阻燃剂制备纳米阿立哌唑生物凝胶及性能评价
本研究旨在以樟科植物Cinnamomum verum j.p rel Syn. C. zeylanicum作为经颅给药的生物阻燃剂和生物稳定剂,制备并评价阿立哌唑生物凝胶。阿立哌唑是一种部分多巴胺激动剂,是一种抗精神病药物,用于治疗精神分裂症、双相情感障碍、重度抑郁症和与自闭症相关的易怒。通过添加最佳量的丙酮,分离出C. verum的生物聚合物,并将其作为生物阻燃剂和生物稳定剂制备负载阿立哌唑的生物凝胶。以葡萄糖和葡聚糖为纳米剂,不同比例的生物聚合物verum(0.4%、0.6%、0.8%和1%)和guargum(1.5%和2%)作为生物阻燃剂,通过优化超声循环制备了初始的阿立哌唑纳米颗粒。将纳米颗粒均匀掺入由海藻酸钠(100 mg)、PVA (100 mg)和HPMC (100 mg)制备的凝胶中,通过pH、结构、展布性、包封率、纳米粒径分布的初步测定和体外药物释放研究等参数的比较,确定制备的生物凝胶为最佳配方。含阻燃剂的FC3(1:0.8)涂覆均匀,质地光滑,51 h时T50%, 72 h时T80%。这些配方可用于经颅药物输送,通过皮肤层、脑膜、三叉神经、输送静脉、颅骨和缝合线将分子靶向到大脑。
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