Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions
This study aimed to prepare an o/w mitiglinide microemulsion (MTGME) to improve the drug solubility and bioavailability. The formulation of o/w MTGME was optimized by the solubility study of drug, pseudo-ternary phase diagram and Box-Behnken design successively. MTGME was characterized by dynamic la...
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| Format: | Article |
| Language: | English |
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Elsevier
2024-01-01
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| Series: | Saudi Pharmaceutical Journal |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1319016423004140 |
| _version_ | 1827344844137168896 |
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| author | Miaomiao Wang Hanghang Li Wenzhi Yang |
| author_facet | Miaomiao Wang Hanghang Li Wenzhi Yang |
| author_sort | Miaomiao Wang |
| collection | DOAJ |
| description | This study aimed to prepare an o/w mitiglinide microemulsion (MTGME) to improve the drug solubility and bioavailability. The formulation of o/w MTGME was optimized by the solubility study of drug, pseudo-ternary phase diagram and Box-Behnken design successively. MTGME was characterized by dynamic laser light scattering (DLS), zeta potential and transmission electron microscopy (TEM), moreover, the storage stability, pharmacodynamics and pharmacokinetics were investigated. The optimal prescription for MTGME consisted of Maisine 35–1 (oil), Cremophor EL (surfactant) and propylene glycol (PG, cosurfactant). MTGME with a spherical dimension of 58.1 ± 5.86 nm was stable when stored at 4 °C for 3 months. The blood glucose levers (BGL) of diabetic mice were uniformly and significantly decreased by intragastric (i.g.) administration of 1–4 mg/kg MTGME, in which BGL (i.g. 4 mg/kg MTGME) was reduced by 69% during 24 h. The pharmacokinetics study of MTGME (i.g., 20 mg/kg) in Wistar rats showed higher plasma drug concentration (Cmax, 2.9 folds), larger area under curve (AUC, 4.6 folds) and oral bioavailability than those of MTG suspensions. Generally, the MTGME (o/w) showed good effect on controlling hyperglycemia. Therefore, microemulsion can be used as an effective oral drug delivery system to improve the bioavailability of MTG. |
| first_indexed | 2024-03-07T22:55:26Z |
| format | Article |
| id | doaj.art-8d12f984a39c43e1afeadeb8d82404c2 |
| institution | Directory Open Access Journal |
| issn | 1319-0164 |
| language | English |
| last_indexed | 2024-03-07T22:55:26Z |
| publishDate | 2024-01-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Saudi Pharmaceutical Journal |
| spelling | doaj.art-8d12f984a39c43e1afeadeb8d82404c22024-02-23T04:58:44ZengElsevierSaudi Pharmaceutical Journal1319-01642024-01-01321101919Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsionsMiaomiao Wang0Hanghang Li1Wenzhi Yang2Department of Pharmacy, Baoding NO. 1 Central Hospital, Baoding Great Wall North Street No. 320, Hebei Province, Baoding 071000, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province & College of Pharmaceutical Science, Hebei University, Baoding 071002, ChinaKey Laboratory of Pharmaceutical Quality Control of Hebei Province & College of Pharmaceutical Science, Hebei University, Baoding 071002, China; Corresponding author at: Hebei University, 180 East Wusi Road, Baoding, Hebei Province 071002, China.This study aimed to prepare an o/w mitiglinide microemulsion (MTGME) to improve the drug solubility and bioavailability. The formulation of o/w MTGME was optimized by the solubility study of drug, pseudo-ternary phase diagram and Box-Behnken design successively. MTGME was characterized by dynamic laser light scattering (DLS), zeta potential and transmission electron microscopy (TEM), moreover, the storage stability, pharmacodynamics and pharmacokinetics were investigated. The optimal prescription for MTGME consisted of Maisine 35–1 (oil), Cremophor EL (surfactant) and propylene glycol (PG, cosurfactant). MTGME with a spherical dimension of 58.1 ± 5.86 nm was stable when stored at 4 °C for 3 months. The blood glucose levers (BGL) of diabetic mice were uniformly and significantly decreased by intragastric (i.g.) administration of 1–4 mg/kg MTGME, in which BGL (i.g. 4 mg/kg MTGME) was reduced by 69% during 24 h. The pharmacokinetics study of MTGME (i.g., 20 mg/kg) in Wistar rats showed higher plasma drug concentration (Cmax, 2.9 folds), larger area under curve (AUC, 4.6 folds) and oral bioavailability than those of MTG suspensions. Generally, the MTGME (o/w) showed good effect on controlling hyperglycemia. Therefore, microemulsion can be used as an effective oral drug delivery system to improve the bioavailability of MTG.http://www.sciencedirect.com/science/article/pii/S1319016423004140Mitiglinide microemulsionBioavailabilityPharmacodynamicsPharmacokinetics |
| spellingShingle | Miaomiao Wang Hanghang Li Wenzhi Yang Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions Saudi Pharmaceutical Journal Mitiglinide microemulsion Bioavailability Pharmacodynamics Pharmacokinetics |
| title | Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions |
| title_full | Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions |
| title_fullStr | Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions |
| title_full_unstemmed | Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions |
| title_short | Preparation, in vitro and in vivo evaluation of a novel mitiglinide microemulsions |
| title_sort | preparation in vitro and in vivo evaluation of a novel mitiglinide microemulsions |
| topic | Mitiglinide microemulsion Bioavailability Pharmacodynamics Pharmacokinetics |
| url | http://www.sciencedirect.com/science/article/pii/S1319016423004140 |
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