Entecavir-loaded poly (lactic-co-glycolic acid) microspheres for long-term therapy of chronic hepatitis-B: Preparation and in vitro and in vivo evaluation
| العنوان: | Entecavir-loaded poly (lactic-co-glycolic acid) microspheres for long-term therapy of chronic hepatitis-B: Preparation and in vitro and in vivo evaluation |
|---|---|
| المؤلفون: | Xiuting He, Rongcai Liang, Aiping Wang, Kaoxiang Sun, Maocai Yan, Fenghua Fu, Chunyan Zhang, Wang Huiyun, Hongjie Mu |
| المصدر: | International Journal of Pharmaceutics. 560:27-34 |
| بيانات النشر: | Elsevier BV, 2019. |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Male, Drug, Guanine, Time Factors, Chemistry, Pharmaceutical, media_common.quotation_subject, Pharmaceutical Science, 02 engineering and technology, Antiviral Agents, 030226 pharmacology & pharmacy, Rats, Sprague-Dawley, 03 medical and health sciences, chemistry.chemical_compound, Hepatitis B, Chronic, 0302 clinical medicine, Differential scanning calorimetry, Polylactic Acid-Polyglycolic Acid Copolymer, X-Ray Diffraction, In vivo, medicine, Animals, Particle Size, Glycolic acid, media_common, Drug Carriers, Chromatography, Calorimetry, Differential Scanning, Chemistry, Entecavir, 021001 nanoscience & nanotechnology, Microspheres, In vitro, Rats, Disease Models, Animal, Drug Liberation, PLGA, Microscopy, Electron, Scanning, Particle size, 0210 nano-technology, medicine.drug |
| الوصف: | To avoid severe exacerbations in the load of hepatitis B virus (HBV) as a consequence of discontinuous use of anti-HBV drugs, entecavir (ETV), the first-line anti-HBV drug, was primally formulated as extended-release poly (lactic-co-glycolic acid) microspheres in the present study. Because ETV is slightly soluble in water and in some other organic solvents used for microsphere preparation, methods for solid-microencapsulation were employed to fabricate the ETV microspheres. The optimized microspheres were evaluated for their morphology, particle size, drug loading, in vitro drug release, and in vivo pharmacokinetics in rats. The optimized formulation was found to have a mean particle size of 86 µm and drug loading of 13%. Differential scanning calorimetry and powder X-ray diffraction indicated that ETV existed in crystal, amorphous, and molecular states in the microspheres. In vitro and in vivo release revealed that the dissolution of ETV dominated the release process. The morphology of the microspheres and changes in the morphology during in vitro release were assessed by scanning electron microscopy. The novel ETV-MS described in this study should have great potential for clinical use as an alternative treatment against HBV. |
| تدمد: | 0378-5173 |
| DOI: | 10.1016/j.ijpharm.2019.01.052 |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::87bcedfb259cb24f20f697bbd72793ed https://doi.org/10.1016/j.ijpharm.2019.01.052 |
| Rights: | CLOSED |
| رقم الانضمام: | edsair.doi.dedup.....87bcedfb259cb24f20f697bbd72793ed |
| قاعدة البيانات: | OpenAIRE |
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