Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles
In this study, gliclazide-loaded cubosomal particles were prepared for improving the oral bioavailability and antidiabetic activity of gliclazide. Four formulations of gliclazide-loaded cubosomal nanoparticles dispersions were prepared by the emulsification method using four different concentrations...
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MDPI AG
2021-08-01
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| Series: | Pharmaceuticals |
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| Online Access: | https://www.mdpi.com/1424-8247/14/8/786 |
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| author | Mohamed Nasr Saud Almawash Ahmed Al Saqr Alaa Y. Bazeed Sameh Saber Heba I. Elagamy |
| author_facet | Mohamed Nasr Saud Almawash Ahmed Al Saqr Alaa Y. Bazeed Sameh Saber Heba I. Elagamy |
| author_sort | Mohamed Nasr |
| collection | DOAJ |
| description | In this study, gliclazide-loaded cubosomal particles were prepared for improving the oral bioavailability and antidiabetic activity of gliclazide. Four formulations of gliclazide-loaded cubosomal nanoparticles dispersions were prepared by the emulsification method using four different concentrations of glyceryl monooleate (GMO) and poloxamer 407 (P407) as the stabilizer. The prepared formulations were in vitro and in vivo evaluated. In vitro, the prepared gliclazide-loaded cubosomal dispersions exhibited disaggregated regular poly-angular particles with a nanometer-sized particle range from 220.60 ± 1.39 to 234.00 ± 2.90 nm and entrapped 73.84 ± 3.03 to 88.81 ± 0.94 of gliclazide. In vitro gliclazide release from cubosomal nanoparticles revealed an initially higher drug release during the first 2 h in acidic pH medium; subsequently, a comparatively higher drug release in alkaline medium relative to gliclazide suspension was observed. An in vivo absorption study in rats revealed a two-fold increase in the bioavailability of gliclazide cubosomal formulation relative to plain gliclazide suspension. Moreover, the study of in vivo hypoglycemic activity indicated that a higher percentage reduction in glucose level was observed after the administration of gliclazide cubosomal nanoparticles to rats. In conclusion, gliclazide-loaded cubosomal nanoparticles could be a promising delivery system for improving the oral absorption and antidiabetic activity of gliclazide. |
| first_indexed | 2024-03-10T08:29:41Z |
| format | Article |
| id | doaj.art-dbae314293644566844847fc6866de17 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-03-10T08:29:41Z |
| publishDate | 2021-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-dbae314293644566844847fc6866de172023-11-22T09:11:49ZengMDPI AGPharmaceuticals1424-82472021-08-0114878610.3390/ph14080786Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal NanoparticlesMohamed Nasr0Saud Almawash1Ahmed Al Saqr2Alaa Y. Bazeed3Sameh Saber4Heba I. Elagamy5Department of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 35712, EgyptDepartment of Pharmaceutical Sciences, College of Pharmacy, Shaqra University, Shaqra 15581, Saudi ArabiaDepartment of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi ArabiaDepartment of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 35712, EgyptDepartment of Pharmacology, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 11152, EgyptDepartment of Pharmaceutics, Faculty of Pharmacy, Delta University for Science and Technology, Gamasa 35712, EgyptIn this study, gliclazide-loaded cubosomal particles were prepared for improving the oral bioavailability and antidiabetic activity of gliclazide. Four formulations of gliclazide-loaded cubosomal nanoparticles dispersions were prepared by the emulsification method using four different concentrations of glyceryl monooleate (GMO) and poloxamer 407 (P407) as the stabilizer. The prepared formulations were in vitro and in vivo evaluated. In vitro, the prepared gliclazide-loaded cubosomal dispersions exhibited disaggregated regular poly-angular particles with a nanometer-sized particle range from 220.60 ± 1.39 to 234.00 ± 2.90 nm and entrapped 73.84 ± 3.03 to 88.81 ± 0.94 of gliclazide. In vitro gliclazide release from cubosomal nanoparticles revealed an initially higher drug release during the first 2 h in acidic pH medium; subsequently, a comparatively higher drug release in alkaline medium relative to gliclazide suspension was observed. An in vivo absorption study in rats revealed a two-fold increase in the bioavailability of gliclazide cubosomal formulation relative to plain gliclazide suspension. Moreover, the study of in vivo hypoglycemic activity indicated that a higher percentage reduction in glucose level was observed after the administration of gliclazide cubosomal nanoparticles to rats. In conclusion, gliclazide-loaded cubosomal nanoparticles could be a promising delivery system for improving the oral absorption and antidiabetic activity of gliclazide.https://www.mdpi.com/1424-8247/14/8/786gliclazideBCS class II drugcubosomesbioavailabilityantidiabetic activity |
| spellingShingle | Mohamed Nasr Saud Almawash Ahmed Al Saqr Alaa Y. Bazeed Sameh Saber Heba I. Elagamy Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles Pharmaceuticals gliclazide BCS class II drug cubosomes bioavailability antidiabetic activity |
| title | Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles |
| title_full | Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles |
| title_fullStr | Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles |
| title_full_unstemmed | Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles |
| title_short | Bioavailability and Antidiabetic Activity of Gliclazide-Loaded Cubosomal Nanoparticles |
| title_sort | bioavailability and antidiabetic activity of gliclazide loaded cubosomal nanoparticles |
| topic | gliclazide BCS class II drug cubosomes bioavailability antidiabetic activity |
| url | https://www.mdpi.com/1424-8247/14/8/786 |
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