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Published on: August 15, 2016
Diclofenac-proline nano-co-crystal development, characterization, in vitro dissolution and diffusion study.
Ilma Nugrahani1, Winni Nur Auli1
1School of Pharmacy, Bandung Institute of Technology, Bandung, 40132, Indonesia.
Nano-co-crystallization improves drug solubility and delivery. This study developed nano-diclofenac-proline-co-crystal (NDPC), showing enhanced dissolution and diffusion compared to conventional forms.
Area of Science:
- Pharmaceutical Science
- Nanotechnology
- Materials Science
Background:
- Nanotechnology enhances solubility of active pharmaceutical ingredients.
- Co-crystal discovery is crucial in drug design.
- Nano-co-crystallization combines these for superior drug properties.
Purpose of the Study:
- To develop nano-diclofenac-proline-co-crystal (NDPC).
- To evaluate NDPC formation kinetics.
- To assess dissolution and diffusion improvements of NDPC.
Main Methods:
- Optimized nano-co-crystal production using top-down (wet milling, neat grinding) and bottom-up (globule inversion, fast evaporation microwaving) methods.
- Characterized NDPC using DLS, microscopy (SEM, TEM), DSC, XRD, and FTIR.
- Determined formation kinetics via FTIR analysis of microwaving effects on co-crystal yield.
- Evaluated dissolution using USP type 2 apparatus and diffusion using Franz cells.
Main Results:
- The bottom-up method (fast evaporation microwaving) yielded optimal NDPC (598.2 ± 63.2 nm, PDI 0.278 ± 0.062).
- NDPC formation kinetics followed a first-order reaction.
- NDPC exhibited significantly improved dissolution and diffusion profiles compared to conventional diclofenac-proline co-crystal (DPC).
Conclusions:
- Nano-co-crystallization is a promising strategy for enhancing drug dissolution and diffusion.
- NDPC offers a superior alternative for drug delivery compared to conventional co-crystals.
- The developed methods provide efficient routes for producing nano-co-crystals with improved pharmaceutical characteristics.
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