Co-encapsulation of Rifampicin and Isoniazid in Crude Soybean Lecithin Liposomes

IF 0.8 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY
C. I. Nkanga, X. Noundou, R. B. Walker, R. Krause
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引用次数: 4

Abstract

Despite the well-known anti-mycobacterial actions of isoniazid (INH) and rifampicin (RIF), the clinical success of tuberculosis (TB) therapy requires prolonged administration of multiple drugs in high doses, which often result in frequent adverse effects and low patient adherence. Although liposomes are promising candidates for controlled delivery of anti-TB drug, the high cost of synthetic and highly purified natural lipids currently used in liposomal technology might preclude the universal application of therapeutic liposomes. This work aimed at evaluating the potential of a cost-effective lipid material, crude soybean lecithin (CL), to co-encapsulate RIF and INH for liposomal dual delivery. RIF was encapsulated in CL-liposomes with/without cholesterol using film hydration method, after which INH was incorporated using a freeze–thawing technique. Dynamic light scattering, differential scanning calorimetry, X-ray diffraction and dialysis were used for liposome characterization. Liposomes containing CL alone (CLL) exhibited 90 % encapsulation efficiency for RIF and 59 % for INH. The mean size and surface charge of CLL were 1114 nm and –63 mV, respectively. In addition, CLL showed a controlled release profile for the co-encapsulated drugs. CLL would be promising vehicles for macrophage-targeting drug delivery. The present findings demonstrate the feasibility of using CL for preparation of combination products for liposomal delivery.
利福平与异烟肼在粗大豆卵磷脂脂质体中的共包封
尽管异烟肼(INH)和利福平(RIF)具有众所周知的抗分枝杆菌作用,但结核病(TB)治疗的临床成功需要长时间高剂量使用多种药物,这往往导致频繁的不良反应和患者的低依从性。虽然脂质体是抗结核药物控制递送的有希望的候选物,但目前脂质体技术中使用的合成和高度纯化的天然脂质体的高成本可能阻碍了治疗性脂质体的普遍应用。这项工作旨在评估一种具有成本效益的脂质材料,粗大豆卵磷脂(CL)的潜力,以共包封RIF和INH进行脂质体双重递送。采用膜水化法将RIF包封在含/不含胆固醇的cl -脂质体中,然后采用冻融技术将INH掺入。动态光散射、差示扫描量热法、x射线衍射和透析等方法对脂质体进行表征。单含CL的脂质体对RIF的包封率为90%,对INH的包封率为59%。CLL的平均尺寸为1114 nm,表面电荷为-63 mV。此外,CLL对共包膜药物表现出控释特征。CLL有望成为巨噬细胞靶向药物递送的载体。本研究结果证明了利用氯代酚制备脂质体联合制剂的可行性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
CiteScore
3.10
自引率
0.00%
发文量
6
审稿时长
>12 weeks
期刊介绍: Original work in all branches of chemistry is published in the South African Journal of Chemistry. Contributions in English may take the form of papers, short communications, or critical reviews.
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