Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics
Introduction: In previous studies carried out in our laboratory, a bile acid (BA) formulation exerted a hypoglycaemic effect in a rat model of type-1 diabetes (T1D). When the antidiabetic drug gliclazide (G) was added to the bile acid, it augmented the hypoglycaemic effect. In a recent study, we des...
| Main Authors: | , , , , , , , , , , , |
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| Format: | Journal Article |
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Springer New York LLC
2014
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| Subjects: | |
| Online Access: | http://hdl.handle.net/20.500.11937/14090 |
| _version_ | 1848748527741566976 |
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| author | Mooranian, Armin Negrulj, Rebecca Mathavan, Sangeetha Martinez, Jorge Sciarretta, Jessica Chen-Tan, Nigel Mukkur, Trilochan Mikov, Momir Lalic-Popovic, M. Stojancevic, M. Golocorbin-Kon, S. Al-Salami, Hani |
| author_facet | Mooranian, Armin Negrulj, Rebecca Mathavan, Sangeetha Martinez, Jorge Sciarretta, Jessica Chen-Tan, Nigel Mukkur, Trilochan Mikov, Momir Lalic-Popovic, M. Stojancevic, M. Golocorbin-Kon, S. Al-Salami, Hani |
| author_sort | Mooranian, Armin |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | Introduction: In previous studies carried out in our laboratory, a bile acid (BA) formulation exerted a hypoglycaemic effect in a rat model of type-1 diabetes (T1D). When the antidiabetic drug gliclazide (G) was added to the bile acid, it augmented the hypoglycaemic effect. In a recent study, we designed a new formulation of gliclazide-cholic acid (G-CA), with good structural properties, excipient compatibility and exhibits pseudoplastic-thixotropic characteristics. The aim of this study is to test the slow release and pH-controlled properties of this new formulation. The aim is also to examine the effect of CA on G release kinetics at various pH values and different temperatures. Method: Microencapsulation was carried out using our Buchi-based microencapsulating system developed in our laboratory. Using sodium alginate (SA) polymer, both formulations were prepared: G-SA (control) and G-CA-SA (test) at a constant ratio (1:3:30), respectively. Microcapsules were examined for efficiency, size, release kinetics, stability and swelling studies at pH 1.5, pH 3, pH 7.4 and pH 7.8 and temperatures of 20 and 30 °C. Results: The new formulation is further optimised by the addition of CA. CA reduced microcapsule swelling of the microcapsules at pH 7.8 and pH 3 at 30 °C and pH 3 at 20 °C, and, even though microcapsule size remains similar after CA addition, percent G release was enhanced at high pH values (pH 7.4 and pH 7.8, p < 0.01). Conclusion: The new formulation exhibits colon-targeted delivery and the addition of CA prolonged G release suggesting its suitability for the sustained and targeted delivery of G and CA to the lower intestine. |
| first_indexed | 2025-11-14T07:06:28Z |
| format | Journal Article |
| id | curtin-20.500.11937-14090 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T07:06:28Z |
| publishDate | 2014 |
| publisher | Springer New York LLC |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-140902017-09-13T15:02:44Z Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics Mooranian, Armin Negrulj, Rebecca Mathavan, Sangeetha Martinez, Jorge Sciarretta, Jessica Chen-Tan, Nigel Mukkur, Trilochan Mikov, Momir Lalic-Popovic, M. Stojancevic, M. Golocorbin-Kon, S. Al-Salami, Hani Bile acid Gliclazide Artificial-cell microencapsulation Diabetes Introduction: In previous studies carried out in our laboratory, a bile acid (BA) formulation exerted a hypoglycaemic effect in a rat model of type-1 diabetes (T1D). When the antidiabetic drug gliclazide (G) was added to the bile acid, it augmented the hypoglycaemic effect. In a recent study, we designed a new formulation of gliclazide-cholic acid (G-CA), with good structural properties, excipient compatibility and exhibits pseudoplastic-thixotropic characteristics. The aim of this study is to test the slow release and pH-controlled properties of this new formulation. The aim is also to examine the effect of CA on G release kinetics at various pH values and different temperatures. Method: Microencapsulation was carried out using our Buchi-based microencapsulating system developed in our laboratory. Using sodium alginate (SA) polymer, both formulations were prepared: G-SA (control) and G-CA-SA (test) at a constant ratio (1:3:30), respectively. Microcapsules were examined for efficiency, size, release kinetics, stability and swelling studies at pH 1.5, pH 3, pH 7.4 and pH 7.8 and temperatures of 20 and 30 °C. Results: The new formulation is further optimised by the addition of CA. CA reduced microcapsule swelling of the microcapsules at pH 7.8 and pH 3 at 30 °C and pH 3 at 20 °C, and, even though microcapsule size remains similar after CA addition, percent G release was enhanced at high pH values (pH 7.4 and pH 7.8, p < 0.01). Conclusion: The new formulation exhibits colon-targeted delivery and the addition of CA prolonged G release suggesting its suitability for the sustained and targeted delivery of G and CA to the lower intestine. 2014 Journal Article http://hdl.handle.net/20.500.11937/14090 10.1007/s12247-014-9182-5 Springer New York LLC fulltext |
| spellingShingle | Bile acid Gliclazide Artificial-cell microencapsulation Diabetes Mooranian, Armin Negrulj, Rebecca Mathavan, Sangeetha Martinez, Jorge Sciarretta, Jessica Chen-Tan, Nigel Mukkur, Trilochan Mikov, Momir Lalic-Popovic, M. Stojancevic, M. Golocorbin-Kon, S. Al-Salami, Hani Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics |
| title | Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics |
| title_full | Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics |
| title_fullStr | Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics |
| title_full_unstemmed | Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics |
| title_short | Stability and Release Kinetics of an Advanced Gliclazide-Cholic Acid Formulation: The Use of Artificial-Cell Microencapsulation in Slow Release Targeted Oral Delivery of Antidiabetics |
| title_sort | stability and release kinetics of an advanced gliclazide-cholic acid formulation: the use of artificial-cell microencapsulation in slow release targeted oral delivery of antidiabetics |
| topic | Bile acid Gliclazide Artificial-cell microencapsulation Diabetes |
| url | http://hdl.handle.net/20.500.11937/14090 |