磺胺嘧啶脂质体给药系统的研制与评价

S. P., A. Sailaja
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引用次数: 0

摘要

本研究的目的是制备并表征载柳氮磺胺脂质体,以提高药物的生物利用度,减轻药物的不良反应。像炎症性肠病这样的疾病可以用抗炎剂治疗,比如“磺胺硫氮嗪”,它也可以用来治疗溃疡性结肠炎和克罗恩病。磺胺吡啶的生物半衰期为5-10hr;与传统疗法一样,有可能错过剂量。因此,频繁给药对于维持理想的稳态水平是必要的。副作用包括血小板减少、巨幼细胞性贫血、骨髓抑制、叶酸缺乏、男性生育能力受损(少精子症)、5-ASA引起的肠道肾炎、腹泻、头痛和皮疹。磺胺吡啶的生物利用度为15%。这项工作是为了提高生物利用度和减少副作用。本研究的主要目的是通过制定一种脂质体给药系统来提高磺胺嘧啶的溶解度。主要目的是开发一种具有良好稳定性和最高包封效率的脂质体制剂。采用薄膜水化法制备脂质体。通过改变大豆卵磷脂和胆固醇的浓度和药物配比,制备了9种脂质体配方。对所得脂质体进行了表面形貌、FTIR、粒径、zeta电位、药物含量、包封效率和体外扩散研究。在9个脂质体配方中,F3为最佳配方,包封效率为97.8%,zeta电位值为-37.2mV。脂质体遵循一级动力学,具有非粘性扩散途径。该脂质体稳定性好,包封效率高。
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Formulation and Evaluation of Liposomal Drug Delivery System for Sulfasalazine
Aim of the current study is to prepare and characterize sulfasalazine-loaded liposomes to improve the bioavailability of the drug and to lessen the adverse effects of the drug. Diseases like inflammatory bowel disease can be treated by anti-inflammatory agents like “Sulfasalazine,” It can also be used to treat ulcerative colitis and Crohn’s disease. The biological half-life of sulfasalazine is 5-10hr; as in the case of conventional therapy, there is a chance of missing the dose. Therefore, frequent administration of drugs is essential to maintain the desired steady-state level. The side effects are thrombocytopenia, megaloblastic anemia, bone marrow depression, folic acid deficiency, impairment of male fertility (Oligospermia), intestinal nephritis due to 5-ASA, diarrhoea, headache, and skin rashes. The bioavailability of sulfasalazine is 15%. This work was undertaken to enhance bioavailability and decrease the side effects. The main objective of the study is to improve the solubility of sulfasalazine by formulating a liposomal drug delivery system. The major objective is to develop a liposomal formulation with good stability and the highest entrapment efficiency. Liposomes were produced by the thin-film hydration method. Nine formulations of liposomes were prepared by varying the concentrations of soya lecithin and cholesterol and changing the drug ratio. The obtained liposomes were characterized for surface morphology, FTIR, particle size, zeta potential, drug content, entrapment efficiency, and in-vitro diffusion studies. Among the nine formulations of liposomes, F3 was found to be the best formulation with an entrapment efficiency of 97.8% and a zeta potential value of -37.2mV. Liposomes followed first-order kinetics with a non-fickian diffusion pathway. Sulfasalazine loaded liposomes were prepared with good stability and the highest entrapment efficiency.
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来源期刊
Current Nanomedicine
Current Nanomedicine Medicine-Medicine (miscellaneous)
CiteScore
2.00
自引率
0.00%
发文量
15
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