Formulation, In Vitro Characterization and Anti-Tuberculosis Investigation of Isoniazid NANOCAPSULES.

IF 2.7 4区 医学 Q2 PHARMACOLOGY & PHARMACY
Chekwube A. Ezegbe, Chukwuemeka C. Mbah, Amarachi G. Ezegbe, Ifeanyi S. Ofoefule, EZINNE C. OKORAFOR
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引用次数: 0

Abstract

Purpose

Tuberculosis (TB) is a major cause of mortality worldwide. The most commonly used first-line anti-TB drugs in the treatment of TB are rifampicin and isoniazid. This research aimed to formulate and evaluate the anti-mycobacterium activity of isoniazid (INH) nano capsules against mycobacterium isolates (M. smegmatis and M. bovis).

Methods

Lecithin was extracted from locally sourced soybean (Glycine max) by aqueous degumming method. Nanoparticles of INH were prepared by mechanical dispersion method. Chitosan was dispersed in 100 mL of acetic acid solution in distilled water overnight. Sodium tripolyphosphate (STPP) was dissolved in 10 mL of distilled water, and added to the chitosan dispersion and stirred using magnetic stirrer at 100 rpm for 30 min. The chitosan/STPP solution and Labrasol® (0.2%), was then added to the organic solution in drops using a syringe and stirred at 10,000 rpm for 45 min using Ultra-turax homogenizer. Subsequently, the precipitate formed was collected after 3 h by centrifugation at 4000 rpm. Nanoparticles obtained were adsorbed by mixing with Neusilin® (0.5%) to form powdered products. Preformulation studies were done using Fourier Transform Infra-Red (FTIR) spectroscopy, Differential Scanning Calorimetry (DSC) and Design Expert®. The nano formulations were characterized for particle size using zeta sizer, morphology by scanning electron microscopy (SEM), thermal properties, entrapment efficiency (EE) and in vitro release.

Results

The percentage yield of the extracted lecithin ranged from 31.0 ± 0.31% to 35.0 ± 0.32%. The DSC thermograph of pure INH was 168.0 °C. The drug content of INH formulation with extracted lecithin (IEL) and isoniazid formulation with reference lecithin (IRL) ranged from 96.4 ± 0.29% to 93.5 ± 0.94% respectively. Encapsulation efficiency for both IEL and IRL were 95.40 ± 0.37% and 95.70 ± 0.10% respectively. INH nano capsule formulations showed significantly (p < 0.05) lower MICs (0.03 μg/mL) than the reference commercial nano capsule (0.05 and 0.10 μg/mL) against M. smegmatis and M. bovis isolates, respectively.

Conclusion

The mycobacterium assay verified that the INH nano capsules had higher potential of activity against the mycobacterial isolates than the conventional nanocapsules. The higher activity may be attributed to increased permeation of the bacterial cell wall, because Labrasol® was used as a permeation enhancer.

Abstract Image

异烟肼纳米胶囊的制备、体外表征及抗结核研究。
目的结核病(TB)是世界范围内死亡的一个主要原因。治疗结核病最常用的一线抗结核药物是利福平和异烟肼。本研究旨在制备并评价异烟肼(INH)纳米胶囊对耻垢分枝杆菌和牛分枝杆菌的抑菌活性。方法采用水脱胶法从本地大豆中提取卵磷脂(Glycine max)。采用机械分散法制备了INH纳米颗粒。壳聚糖分散于100 mL醋酸溶液中,在蒸馏水中过夜。将三聚磷酸钠(STPP)溶解于10 mL蒸馏水中,加入壳聚糖分散液中,用磁力搅拌器以100 rpm搅拌30 min。然后用注射器将壳聚糖/STPP溶液和Labrasol®(0.2%)滴入有机溶液中,并使用Ultra-turax均质机以10,000 rpm搅拌45 min。随后,在4000 rpm离心3 h后收集形成的沉淀物。获得的纳米颗粒通过与Neusilin®(0.5%)混合吸附形成粉末状产品。配方前研究使用傅里叶变换红外光谱(FTIR),差示扫描量热法(DSC)和Design Expert®。采用zeta粒度仪、扫描电镜(SEM)、热性能、包埋效率(EE)和体外释放度对纳米配方进行了表征。结果提取的卵磷脂提取率范围为31.0±0.31% ~ 35.0±0.32%。纯INH的DSC热像图为168.0℃。含提取卵磷脂的INH制剂(IEL)和含参比卵磷脂的异烟肼制剂(IRL)的药物含量分别为96.4±0.29% ~ 93.5±0.94%。el和IRL的包封率分别为95.40±0.37%和95.70±0.10%。INH纳米胶囊制剂对耻垢分枝杆菌和牛分枝杆菌分离株的mic值(0.03 μg/mL)显著低于对照市售纳米胶囊(0.05和0.10 μg/mL) (p < 0.05)。结论INH纳米胶囊对分离的分枝杆菌具有较强的抑菌活性。较高的活性可能是由于增加了细菌细胞壁的渗透性,因为Labrasol®被用作渗透性增强剂。
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
Journal of Pharmaceutical Innovation
Journal of Pharmaceutical Innovation PHARMACOLOGY & PHARMACY-
CiteScore
3.70
自引率
3.80%
发文量
90
审稿时长
>12 weeks
期刊介绍: The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories: Materials science, Product design, Process design, optimization, automation and control, Facilities; Information management, Regulatory policy and strategy, Supply chain developments , Education and professional development, Journal of Pharmaceutical Innovation publishes four issues a year.
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