دورية أكاديمية
Modification of microenvironmental pH of nanoparticles for enhanced solubility and oral bioavailability of poorly water-soluble celecoxib.
| العنوان: | Modification of microenvironmental pH of nanoparticles for enhanced solubility and oral bioavailability of poorly water-soluble celecoxib. |
|---|---|
| المؤلفون: | Ran Woo M; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Bak YW; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Cheon S; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Suk Kim J; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Hun Ji S; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Park S; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Woo S; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea., Oh Kim J; College of Pharmacy, Yeungnam University, 214-1, Dae-Dong, Gyongsan 712-749, South Korea., Giu Jin S; Department of Pharmaceutical Engineering, Dankook University, 119 Dandae-ro, Dongnam-gu, Cheonan 31116, South Korea. Electronic address: sklover777@dankook.ac.kr., Choi HG; College of Pharmacy, Hanyang University, 55 Hanyangdaehak-ro, Sangnok-gu, Ansan 15588, South Korea. Electronic address: hangon@hanyang.ac.kr. |
| المصدر: | International journal of pharmaceutics [Int J Pharm] 2024 Jun 25; Vol. 659, pp. 124179. Date of Electronic Publication: 2024 Apr 29. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: Elsevier/North-Holland Biomedical Press Country of Publication: Netherlands NLM ID: 7804127 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1873-3476 (Electronic) Linking ISSN: 03785173 NLM ISO Abbreviation: Int J Pharm Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Amsterdam, Elsevier/North-Holland Biomedical Press. |
| مواضيع طبية MeSH: | Celecoxib*/pharmacokinetics , Celecoxib*/administration & dosage , Celecoxib*/chemistry , Solubility* , Biological Availability* , Nanoparticles*/chemistry , Rats, Sprague-Dawley* , Water*/chemistry, Animals ; Hydrogen-Ion Concentration ; Male ; Administration, Oral ; Rats ; Particle Size ; Cyclooxygenase 2 Inhibitors/pharmacokinetics ; Cyclooxygenase 2 Inhibitors/administration & dosage ; Cyclooxygenase 2 Inhibitors/chemistry |
| مستخلص: | This study aimed to develop a novel pH-modified nanoparticle with improved solubility and oral bioavailability of poorly water-soluble celecoxib by modifying the microenvironmental pH. After assessing the impact of hydrophilic polymers, surfactants and alkaline pH modifiers on the drug solubility, copovidone, sodium lauryl sulfate (SLS) and meglumine were chosen. The optimal formulation of solvent-evaporated, surface-attached and pH-modified nanoparticles composed of celecoxib/copovidone/SLS/meglumine at weight ratios of 1:1:0.2:0, 1:0.375:1.125:0 and 1:1:1:0.2:0.02, respectively, were manufactured using spray drying technique. Their physicochemical characteristics, solubility, dissolution and pharmacokinetics in rats were evaluated compared to the celecoxib powder. The solvent-evaporated and pH-modified nanoparticles converted a crystalline to an amorphous drug, resulting in a spherical shape with a reduced particle size compared to celecoxib powder. However, the surface-attached nanoparticles with insignificant particle size exhibited the unchangeable crystalline drug. All of them gave significantly higher solubility, dissolution, and oral bioavailability than celecoxib powder. Among them, the pH-modified nanoparticles demonstrated the most significant improvement in solubility (approximately 1600-fold) and oral bioavailability (approximately 4-fold) compared to the drug powder owing to the alkaline microenvironment formation effect of meglumine and the conversion to the amorphous drug. Thus, the pH-modified nanoparticle system would be a promising strategy for improving the solubility and oral bioavailability of poorly water-soluble and weakly acidic celecoxib. Competing Interests: Declaration of competing interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper. (Copyright © 2024 Elsevier B.V. All rights reserved.) |
| فهرسة مساهمة: | Keywords: Celecoxib; Crystallinity; Oral bioavailability; Solubility; pH-modified nanoparticles |
| المشرفين على المادة: | JCX84Q7J1L (Celecoxib) 059QF0KO0R (Water) 0 (Cyclooxygenase 2 Inhibitors) |
| تواريخ الأحداث: | Date Created: 20240501 Date Completed: 20240615 Latest Revision: 20240615 |
| رمز التحديث: | 20240616 |
| DOI: | 10.1016/j.ijpharm.2024.124179 |
| PMID: | 38692498 |
| قاعدة البيانات: | MEDLINE |
Full Text Finder | تدمد: | 1873-3476 |
|---|---|
| DOI: | 10.1016/j.ijpharm.2024.124179 |