NANOCRYSTALLIZATION OF DAPSONE; A NOVEL APPROACH TO BOOST SOLUBILITY, DISSOLUTION, AND IN-VITRO ANTI-INFLAMMATORY ACTIVITY | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Article 1, Volume 66, Issue 2, September and October 2022, Pages 1-28 PDF (985.97 K) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajps.2022.268247 | ||
| Authors | ||
| Gamal Zayed* 1; Hanaa Mohammed2; Shaaban Osman3 | ||
| 1Faculty f Pharmacy, AlAzhar University | ||
| 2Pharmacist at Al-Azhar University Hospital, Assiut 71524, Egypt. | ||
| 3Al-Azhar Center of Nanosciences and Applications (ACNA), Al-Azhar University, Assiut 71524, Egypt. | ||
| Abstract | ||
| The low aqueous solubility of dapsone (DPS), a widely used anti-acne drug, greatly limits its biological efficacy, especially the anti-inflammatory effect. This article has applied the nanocrystallization technique to increase the surface area which consequently improves the solubility, dissolution, and anti-inflammatory effect of dapsone. Span-stabilized dapsone nanocrystals (DPS-NCs) have been prepared using solvent-antisolvent crystallization technique. The obtained nanocrystals (NCs) were characterized by FTIR, DSC, and X-ray. The morphology, particles surface, sizes, and surface charge of DPS-NCs were examined by TEM, SEM, and zetasizer, respectively. Additionally, the in vitro solubility, dissolution, and anti-inflammatory of the DPS-NCs were investigated. DPS-NCs were spherical in shape with smooth surfaces and had a hydrodynamic particle size of about 149±4.73 nm. The saturated aqueous solubility of DPS-NCs was 1.8 ± 0.05 mg/mL which was about 6 fold higher than that of a pure drug and showed improved in vitro dissolution. The used excipients did not interact chemically with the drug as indicated by DSC and FTIR. X-ray diffraction and TEM imaging confirmed that the produced nanocrystals (NCs) still have a certain degree of crystallinity and did not completely convert to the amorphous state. The in vitro anti-inflammatory of DPS-NCs greatly improved compared to pure drug. DSP-NCs could be considered a novel, promising, and effective therapeutic option for the treatment of acne as well as for relieving the accompanying inflammation. | ||
| Keywords | ||
| Dapsone nanocrystal; solvent-antisolvent; solubility; dissolutions; in vitro anti-inflammatory | ||
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