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Optimizing formulation parameters for the development of carvedilol injectable in situ forming depots
Majd Alrashdan1, Ziad A Shraideh2, Samer R Abulateefeh1
1School of Pharmacy, The University of Jordan, Amman, Jordan.
Pharmaceutical Development and Technology
|October 5, 2023
Summary
This study developed a new injectable long-acting carvedilol in situ forming depot (ISFD) system. The polymer choice allowed tunable drug release over 30 days, offering a promising alternative for chronic condition management.
Area of Science:
- Biomedical Engineering
- Materials Science
- Pharmaceutical Sciences
Background:
- Conventional sustained drug delivery systems face limitations.
- Carvedilol, a daily medication for chronic conditions, has a short half-life.
- Injectable in situ forming depots (ISFDs) offer an alternative drug delivery approach.
Purpose of the Study:
- To develop and characterize a novel injectable long-acting carvedilol-ISFD formulation.
- To evaluate the impact of polymer properties (lactide-to-glycolide ratio and end-functionality) on ISFD performance.
- To investigate the influence of organic solvents on depot formation and drug release.
Main Methods:
- Four grades of polyesters (PLGA and PLA with acid- or ester-capping) were used to prepare ISFDs.
- Various organic solvents (NMP, DMSO, ethyl acetate, benzyl benzoate) were screened for depot formation.
- Encapsulation efficiency and in vitro drug release profiles over 30 days were assessed.
Main Results:
- N-methyl-2-pyrrolidone (NMP) and dimethyl sulfoxide (DMSO) proved suitable for depot formation.
- All ISFD formulations achieved high encapsulation efficiencies (96-98%).
- PLGA-based ISFDs extended carvedilol release over 30 days, while PLA-based ISFDs showed slower release (36-60%).
Conclusions:
- Injectable carvedilol-ISFDs were successfully developed with tunable extended-release properties.
- The choice of polymer grade (PLGA vs. PLA, end-capping) significantly influenced drug release kinetics.
- This technology presents a novel injectable formulation for long-acting carvedilol delivery.
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