Enhancing the oral bioavailability of fisetin: polysaccharide-based self nano-emulsifying spheroids for colon-targeted delivery.

Autor: Gunjal P; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India., Vishwas S; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India., Kumar R; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India., Bashir B; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India., Kumar B; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India., Khurana N; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India., Gulati M; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India.; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW, 2007, Australia., Gupta G; Centre for Global Health Research, Saveetha Medical College, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, India.; Centre of Medical and Bio-Allied Health Sciences Research, Ajman University, Ajman, United Arab Emirates., Prasher P; Department of Chemistry, University of Petroleum & Energy Studies, Energy Acres, Dehradun, 248007, India., Kumbhar P; Department of Pharmaceutics, Tatyasaheb Kore College of Pharmacy, Warananagar, Tal: Panhala, Dist: Kolhapur, Maharashtra, 416113, India., Disouza J; Department of Pharmaceutics, Tatyasaheb Kore College of Pharmacy, Warananagar, Tal: Panhala, Dist: Kolhapur, Maharashtra, 416113, India., Kuppusamy G; Department of Pharmaceutics, JSS College of Pharmacy, JSS Academy of Higher Education & Research, Ooty, Nilgiris, India., Mohammed Y; Faculty of Medicine, Frazer Institute, The University of Queensland, Brisbane, QLD, 4102, Australia.; School of Pharmacy, The University of Queensland, Brisbane, QLD, 4102, Australia., Dureja H; Department of Pharmaceutical Sciences, Maharshi Dayanand University, Rohtak, Haryana, 124001, India., Dua K; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW, 2007, Australia.; Discipline of Pharmacy, Graduate School of Health, University of Technology Sydney, Ultimo, NSW, 2007, Australia., Singh SK; School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, Punjab, India. singhsachin23@gmail.com.; Faculty of Health, Australian Research Centre in Complementary and Integrative Medicine, University of Technology Sydney, Ultimo, NSW, 2007, Australia. singhsachin23@gmail.com.
Jazyk: angličtina
Zdroj: Drug delivery and translational research [Drug Deliv Transl Res] 2024 Oct; Vol. 14 (10), pp. 1-17. Date of Electronic Publication: 2024 May 24.
DOI: 10.1007/s13346-024-01634-6
Abstrakt: Fisetin (FS) is a flavonoid that possesses antioxidant and anti-inflammatory properties against ulcerative colitis. FS shows poor dissolution rate and permeability. An attempt has been made to develop colon-targeted solid self-nanoemulsifying drug delivery systems (S-SNEDDS) of FS. Initially, liquid (L) SNEDDS were prepared by loading FS into isotropic mixture of L-SNEDDS was prepared using Labrafil M 1944 CS, Transcutol P, and Tween 80. These L-SNEDDS were further converted into solid (S) SNEDDS by mixing the isotropic mixture with 1:1:1 ratio of guar gum (GG), xanthan gum (XG) and pectin (PC) [GG:XG:PC (1:1:1)]. Aerosil-200 (A-200) was added to enhance their flow characteristics. Further, they were converted into spheroids by extrusion-spheronization technique. The solid-state characterization of S-SNEDDS was done by SEM, DSC, and PXRD, which revealed that the crystalline form of FS was converted into the amorphous form. In the dissolution study, S-SNEDDS spheroids [GG:XG:PC (1:1:1)] exhibited less than 20% drug release within the first 5 h, followed by rapid release of the drug between the 5th and 10th h, indicating its release at colonic site. The site-specific delivery of FS to colon via FS-S-SNEDDS spheroids was confirmed by conducting pharmacokinetic studies on rats. Wherein, results showed delay in absorption of FS loaded in spheroids up to 5 h and achievement of Cmax at 7h, whereas L-SNEDDS showed rapid absorption of FS. Furthermore, FS-L-SNEDDS and FS-S-SNEDDS spheroids [GG:XG:PC (1:1:1)] increased oral bioavailability of FS by 6.86-fold and 4.44-fold, respectively, as compared to unprocessed FS.
(© 2024. Controlled Release Society.)
Databáze: MEDLINE
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