Transdermal Delivery of Lornoxicam Hybrid Nanogel: Design, Preparation, Characterization, and In-Vitro Diffusion Evaluation

Hayder Kadhim Drais
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Abstract

Lornoxicam was practically water insoluble and a nonsteroidal anti-inflammatory therapeutic agent thus associated with gastrointestinal tract (GIT) side effects. Lipid polymer hybrid nanocarriers (LPHNs)-based transdermal nanogel of lornoxicam was formulated to increase solubility of lornoxicam and sustained lornoxicam release that lead to eliminate GIT related side effect, prolong therapeutic activity and improve patient compliance .The lornoxicam LPHNs formulations (LH1-LH6) were prepared by microwaves based method. The conventional gel of lornoxicam (G) was prepared by solvent diffusion method. The LH1-LH6 was entered to characterization processes that were later used as a base to prepare lornoxicam hybrid nanogel formulations (LN1-LN6). The LN1-LN6 was tested for various evaluations. It was found that all the LH1-LH6 were show nanosize globules, low polydispersity index and acceptable surface charge, entrapment efficiency and drug loading. LH3 was the most optimized LPHNs due had lower particle size and higher lornoxicam release.The evaluation processes indicate stable organoleptic properties, high homogeneity, and acceptable values of pH. The comparability profile of the lornoxicam release from the lornoxicam nanogel formulations (LN1-LN6) and conventional lornoxicam gel (G) was in the following descending order: LN3 > LN2> LN1 > LN6 > LN5 > LN4 > G. The characterization and evaluation processes highly support promise transdermal delivery system to decrease pain and inflammation in musculoskeletal diseases.
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氯诺昔康混合纳米凝胶的透皮递送:设计、制备、表征和体外扩散评价
氯诺昔康几乎不溶于水,是一种非甾体抗炎治疗剂,因此与胃肠道(GIT)副作用有关。采用微波法制备氯诺昔康脂质聚合物杂化纳米载体(LPHNs)透皮纳米凝胶,以提高氯诺昔康的溶解度和缓释氯诺昔康,消除GIT相关副作用,延长治疗活性,提高患者依从性。采用溶剂扩散法制备氯诺昔康常规凝胶。LH1-LH6进入表征过程,随后用作制备氯诺昔康杂化纳米凝胶制剂(LN1-LN6)的基础。LN1-LN6进行了各种评估测试。结果表明,LH1-LH6均呈纳米级球状,多分散性指数低,表面电荷、包载效率和载药量均可接受。LH3粒径较小,氯诺昔康释放量较大,是最佳的lphn。评价过程表明,氯诺昔康的感官性能稳定,均匀性高,ph值可接受。氯诺昔康纳米凝胶制剂(LN1-LN6)与常规氯诺昔康凝胶(G)的释放度可比性从高到低依次为:LN3 >LN2>LN1祝辞LN6祝辞LN5祝辞LN4祝辞表征和评估过程高度支持透皮给药系统减少肌肉骨骼疾病的疼痛和炎症。
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