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首页> 外文期刊>Nanobiotechnology, IET >Enhanced efficacy of clindamycin hydrochloride encapsulated in PLA/PLGA based nanoparticle system for oral delivery
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Enhanced efficacy of clindamycin hydrochloride encapsulated in PLA/PLGA based nanoparticle system for oral delivery

机译：包裹在基于PLA / PLGA的纳米颗粒系统中的盐酸克林霉素的口服给药的增强功效

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Clindamycin hydrochloride (CLH) is a clinically important oral antibiotic with wide spectrum of antimicrobial activity that includes gram-positive aerobes (staphylococci, streptococci etc.), most anaerobic bacteria, Chlamydia and certain protozoa. The current study was focused to develop a stabilised clindamycin encapsulated poly lactic acid (PLA)/poly (D,L-lactide-co-glycolide) (PLGA) nano-formulation with better drug bioavailability at molecular level. Various nanoparticle (NPs) formulations of PLA and PLGA loaded with CLH were prepared by solvent evaporation method varying drug: polymer concentration (1:20, 1:10 and 1:5) and characterised (size, encapsulation efficiency, drug loading, scanning electron microscope, differential scanning calorimetry [DSC] and Fourier transform infrared [FTIR] studies). The ratio 1:10 was found to be optimal for a monodispersed and stable nano formulation for both the polymers. NP formulations demonstrated a significant controlled release profile extended up to 144 h (both CLH-PLA and CLH-PLGA). The thermal behaviour (DSC) studies confirmed the molecular dispersion of the drug within the system. The FTIR studies revealed the intactness as well as unaltered structure of drug. The CLH-PLA NPs showed enhanced antimicrobial activity against two pathogenic bacteria Streptococcus faecalis and Bacillus cereus. The results notably suggest that encapsulation of CLH into PLA/PLGA significantly increases the bioavailability of the drug and due to this enhanced drug activity; it can be widely applied for number of therapies.
机译：盐酸克林霉素（CLH）是临床上重要的口服抗生素，具有广泛的抗菌活性，包括革兰氏阳性需氧菌（葡萄球菌，链球菌等），大多数厌氧菌，衣原体和某些原生动物。当前的研究重点是开发稳定的克林霉素包裹的聚乳酸（PLA）/聚（D，L-丙交酯-乙交酯-乙交酯）（PLGA）纳米制剂，在分子水平上具有更好的药物生物利用度。通过溶剂蒸发法制备了不同浓度的药物：聚合物浓度（1：20、1：10和1：5）的PLA和PLGA的PLA和PLGA纳米颗粒制剂，并对其进行了表征（尺寸，包封效率，药物载量，扫描电子）显微镜，差示扫描量热法[DSC]和傅立叶变换红外[FTIR]研究）。对于两种聚合物的单分散且稳定的纳米制剂，发现1:10的比例是最佳的。 NP制剂表现出显着的控释曲线，延长至144小时（CLH-PLA和CLH-PLGA）。热行为（DSC）研究证实了药物在系统中的分子分散性。 FTIR研究揭示了药物的完整性和未改变的结构。 CLH-PLA NPs对两种病原菌粪便链球菌和蜡状芽孢杆菌均显示出增强的抗菌活性。结果特别表明，将CLH封装到PLA / PLGA中可显着提高药物的生物利用度，并且由于这种药物活性增强。它可以广泛应用于多种疗法。

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