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Solid State Characterization and Dissolution Enhancement of Nevirapine Cocrystals
Prabhakar Panzade1, Giridhar Shendarkar2, Deepak Kulkarni1
1Department of Pharmaceutics, Srinath College of Pharmacy, Aurangabad, India.
Advanced Pharmaceutical Bulletin
|December 10, 2021
Summary
Novel cocrystals of nevirapine (NP) were developed using salicylamide and 3-hydroxy benzoic acid (3-HBA). These cocrystals significantly enhanced NP
Area of Science:
- Pharmaceutical Sciences
- Solid-State Chemistry
- Drug Delivery
Background:
- Nevirapine (NP) is an antiretroviral drug with poor solubility and dissolution characteristics.
- Improving the physicochemical properties of NP is crucial for enhancing its therapeutic efficacy.
- Cocrystal formation is a promising strategy for drug property enhancement.
Purpose of the Study:
- To design and prepare novel cocrystals of nevirapine (NP) with salicylamide and 3-hydroxy benzoic acid (3-HBA).
- To investigate the solubility, dissolution rate, and physical stability of the prepared NP cocrystals.
- To evaluate the potential of cocrystal formation for improving NP's pharmaceutical performance.
Main Methods:
- Cocrystals were synthesized using the solvent drop grinding method with acetone.
- Characterization involved differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD).
- Solubility studies were conducted at various pH values, with and without a surfactant (Tween 80). Intrinsic dissolution rate (IDR) and physical stability were also assessed.
Main Results:
- DSC and PXRD confirmed the formation of new solid forms (cocrystals).
- The NP-3-HBA cocrystal exhibited a 4.5-fold increase in solubility at pH 1.2 and a 5.5-fold increase in 1% Tween 80 compared to pure NP.
- Cocrystals demonstrated higher IDR in 0.1 N HCl and remained physically stable for 3 months.
Conclusions:
- Novel, stable cocrystals of nevirapine were successfully prepared.
- Cocrystal formation significantly improved the solubility and dissolution rate of nevirapine.
- These findings suggest cocrystals are a viable approach to enhance nevirapine's drug delivery and therapeutic potential.
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