Chekwube A. Ezegbe, Chukwuemeka C. Mbah, Amarachi G. Ezegbe, Ifeanyi S. Ofoefule, EZINNE C. OKORAFOR
{"title":"异烟肼纳米胶囊的制备、体外表征及抗结核研究。","authors":"Chekwube A. Ezegbe, Chukwuemeka C. Mbah, Amarachi G. Ezegbe, Ifeanyi S. Ofoefule, EZINNE C. OKORAFOR","doi":"10.1007/s12247-025-10030-7","DOIUrl":null,"url":null,"abstract":"<div><h3>Purpose</h3><p>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 (<i>M. smegmatis</i> and <i>M. bovis</i>).</p><h3>Methods</h3><p>Lecithin was extracted from locally sourced soybean (<i>Glycine max</i>) 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<i>.</i> 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.</p><h3>Results</h3><p>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 (<i>p</i> < 0.05) lower MICs (0.03 μg/mL) than the reference commercial nano capsule (0.05 and 0.10 μg/mL) against <i>M. smegmatis</i> and <i>M. bovis</i> isolates, respectively.</p><h3>Conclusion</h3><p>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.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"20 4","pages":""},"PeriodicalIF":2.7000,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Formulation, In Vitro Characterization and Anti-Tuberculosis Investigation of Isoniazid NANOCAPSULES.\",\"authors\":\"Chekwube A. Ezegbe, Chukwuemeka C. Mbah, Amarachi G. Ezegbe, Ifeanyi S. Ofoefule, EZINNE C. OKORAFOR\",\"doi\":\"10.1007/s12247-025-10030-7\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><h3>Purpose</h3><p>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 (<i>M. smegmatis</i> and <i>M. bovis</i>).</p><h3>Methods</h3><p>Lecithin was extracted from locally sourced soybean (<i>Glycine max</i>) 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<i>.</i> 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.</p><h3>Results</h3><p>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 (<i>p</i> < 0.05) lower MICs (0.03 μg/mL) than the reference commercial nano capsule (0.05 and 0.10 μg/mL) against <i>M. smegmatis</i> and <i>M. bovis</i> isolates, respectively.</p><h3>Conclusion</h3><p>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.</p></div>\",\"PeriodicalId\":656,\"journal\":{\"name\":\"Journal of Pharmaceutical Innovation\",\"volume\":\"20 4\",\"pages\":\"\"},\"PeriodicalIF\":2.7000,\"publicationDate\":\"2025-07-05\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Pharmaceutical Innovation\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s12247-025-10030-7\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmaceutical Innovation","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s12247-025-10030-7","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Formulation, In Vitro Characterization and Anti-Tuberculosis Investigation of Isoniazid NANOCAPSULES.
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.
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.