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Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
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Mixed micelles formulation for carvedilol delivery: In-vitro characterization and in-vivo evaluation
Kıvılcım Öztürk1, Fatma Betül Arslan1, Süleyman Can Öztürk2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, 06100 Ankara, Turkey.
International Journal of Pharmaceutics
|November 18, 2021
Summary
This study developed a novel micelle formulation to enhance carvedilol
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Carvedilol (CAR) is an antihypertensive drug with poor water solubility and low oral bioavailability.
- Existing formulations limit carvedilol's therapeutic potential.
- Micellar formulations offer a promising approach to improve drug solubility and pharmacokinetics.
Purpose of the Study:
- To improve the aqueous solubility and pharmacokinetic profile of carvedilol.
- To develop and characterize an optimized self-assembly micelle formulation for carvedilol.
- To evaluate the in vitro dissolution and in vivo pharmacokinetic performance of the micellar formulation.
Main Methods:
- An optimized micelle formulation was prepared using Pluronic® F127, D-α-tocopheryl polyethylene glycol 1000 succinate, and L-cysteine HCl (4:3:3 ratio).
- Characterization included micellar size, polydispersity index, zeta potential, morphology (TEM), critical micelle concentration, and thermal behavior.
- In vitro dissolution studies and in vivo pharmacokinetic studies in rats were conducted.
Main Results:
- Carvedilol's aqueous solubility increased up to 271-fold upon encapsulation in the mixed micelles.
- Micelles exhibited small sizes (<30 nm) and spherical morphology.
- The micellar formulation significantly enhanced carvedilol dissolution and improved pharmacokinetic parameters (t1/2, AUC0-∞) in rats compared to commercial tablets.
Conclusions:
- The optimized micelle formulation effectively enhances carvedilol's solubility and bioavailability.
- This nanocarrier system shows potential for developing improved antihypertensive and cardiovascular disease treatments.
- Further development could lead to novel therapeutic options for hypertension management.
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