Academic Journal
Capryol-ethyl oleate self-microemulsifying system for improved intestinal absorption and hypoglycemic activity of empagliflozin.
| Τίτλος: | Capryol-ethyl oleate self-microemulsifying system for improved intestinal absorption and hypoglycemic activity of empagliflozin. |
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| Συγγραφείς: | Hathout EM; Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt., Eltokhy SS; Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt., Abdelkader DH; Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt., El Maghraby GM; Department of Pharmaceutical Technology, Faculty of Pharmacy, Tanta University, Tanta, Egypt. |
| Πηγή: | Pharmaceutical development and technology [Pharm Dev Technol] 2026 Jun; Vol. 31 (5), pp. 778-793. Date of Electronic Publication: 2026 May 20. |
| Τύπος έκδοσης: | Journal Article |
| Γλώσσα: | English |
| Στοιχεία περιοδικού: | Publisher: Informa Healthcare Country of Publication: England NLM ID: 9610932 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1097-9867 (Electronic) Linking ISSN: 10837450 NLM ISO Abbreviation: Pharm Dev Technol Subsets: MEDLINE |
| Imprint Name(s): | Publication: London : Informa Healthcare Original Publication: Monticello, NY : Marcel Dekker, c1996- |
| Ιατρικοί όροι (MeSH): | Intestinal Absorption*/drug effects , Benzhydryl Compounds*/administration & dosage , Benzhydryl Compounds*/pharmacokinetics , Benzhydryl Compounds*/pharmacology , Hypoglycemic Agents*/administration & dosage , Hypoglycemic Agents*/pharmacokinetics , Hypoglycemic Agents*/pharmacology , Hypoglycemic Agents*/chemistry , Diabetes Mellitus, Experimental*/drug therapy , Glucosides*/administration & dosage , Glucosides*/pharmacokinetics , Glucosides*/pharmacology , Oleic Acids*/chemistry, Emulsions/chemistry ; Drug Delivery Systems/methods ; Blood Glucose/drug effects ; Animals ; Male ; Rats ; Administration, Oral ; Rats, Sprague-Dawley |
| Περίληψη: | Empagliflozin (EMPA) is a poorly permeable oral hypoglycemic agent. It is potential substrate for P-glycoprotein (P-gp). This work assessed the impact of anatomical sites on EMPA intestinal absorption and assessed self-microemulsifying drug delivery systems (SMEDDS) as a novel strategy for augmented intestinal permeability and oral hypoglycemia of EMPA. A pseudo-ternary phase diagram was used to select a nano-formulation encompassing 60% tween 60: 30% transcutol: 5% capryol: 5% ethyl oleate. This was characterized for droplet size which was 31.2 nm, PDI was 0.292, and zeta potential which was -1.2 mV. EMPA absorption was assessed using in situ intestinal absorption, and the system was evaluated in vivo using diabetic rats. In situ intestinal absorption studies from aqueous solutions demonstrated poor permeability of EMPA from all tested segments relating to the regional distribution of P-gp efflux transporters. Perfusion of EMPA as microemulsion resulting from reconstitution of SMEDDS enhanced ileal and colonic absorption by 1.9 and 1.85-fold, respectively. Furthermore, in vivo studies demonstrated significant augmentation in oral hypoglycemic activity of EMPA, revealed as 1.45-fold elevation in area under blood glucose reduction curve after administration of SMEDDS compared to EMPA aqueous dispersion. SMEDDS formulation successfully improved intestinal absorption, hypoglycemic efficacy and hence oral bioavailability of EMPA. |
| Contributed Indexing: | Keywords: BCS class III; Empagliflozin; SMEDDS; diabetic rats; in situ; intestinal absorption |
| Substance Nomenclature: | 0 (Benzhydryl Compounds) 0 (Hypoglycemic Agents) 0 (Emulsions) 0 (Glucosides) HDC1R2M35U (empagliflozin) Z2Z439864Y (ethyl oleate) 0 (Oleic Acids) 0 (Blood Glucose) |
| Entry Date(s): | Date Created: 20260516 Date Completed: 20260727 Latest Revision: 20260727 |
| Update Code: | 20260728 |
| DOI: | 10.1080/10837450.2026.2674731 |
| PMID: | 42143023 |
| Βάση Δεδομένων: | MEDLINE |
| ISSN: | 1097-9867 |
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| DOI: | 10.1080/10837450.2026.2674731 |