Formulation of Nitrendipin Nanocrystals for Solubility and Dissolution Enhancement

The objective of present work was to prepare nanocrystals of Nitrendipin (NTD) to enhance its solubility and dissolution rate with aim of dose reduction and minimising the side effects associated with it's oral administration. The optimised nanocrystals formulation had particle size 335nm, PDI 0.262, practical yield 85%, and ZP in the range of of -20 to -45mv. X-Ray diffraction studies (XRPD) and Differential scanning calorimetry (DSC) studies suggested nanocrystal formation and absence of crystalline peaks, indicating loss of crystallinity, additionally confirmed by scanning electron microscopy (SEM). Nanocrystals showed 30.45 fold enhancements in aqueous solubility, and 38.5 fold in phosphate buffer pH 1.2, as compared to pure NTD. In vitro release studies have demonstrated 96.186% cumulative drug release within 60 min from nanocrystals compared to 22.17% from pure NTD. Stable NTD nanocrystals formulated by anti-solvent precipitation method shows improved solubility and dissolution. It has been concluded that NTD nanocrystals were obtained with significant improvement in saturation solubility and drug losing it's crystalline nature, when compared with plain drug.