Design & Characterization of Nanocrystals of Lovastatin for Solubility & Dissolution Enhancement

1. Design & Characterization of Nanocrystals of Lovastatin for Solubility & Dissolution Enhancement Dr. Basavaraj K. NanjwadeM. Pharm, PhD. Department of Pharmaceutics KLE University’s College of Pharmacy Belgaum-590010 E-mail: bknanjwade@yahoo.co.in Cell No: 00919742431000

2. Introduction • Nanocrystal • Definition: • Drug nanocrystals are nanoparticles being composed of 100% drug without any matrix material. • Methods of production: - Bottom up technology: Precipitation - Top down technology: High pressure homogenization NIPER, Chandigarh

3. Objectives of the study: • To increase the drug solubility & dissolution. • To increase the drug bioavailability. • Materials & Methods: • Materials: • Drug: Lovastatin (Kreb’s biochemicals Pvt. Ltd., Hyderabad) • Solvents: Acetone, Methanol, Acetonitrile NIPER, Chandigarh

4. Method: • All the formulations were prepared by Precipitation method. Involves two steps….. • Preparation of drug solution in solvent • Addition of drug solution to water NIPER, Chandigarh

5. Nanocrystal preparation NIPER, Chandigarh

6. Evaluation parameters a) Particle morphology b) Particle size analysis c) Crystalline state evaluation - Powder X-ray diffraction (PXRD) - Differential scanning calorimetry (DSC) d) Solubility determination e) In vitro release study f) In vivo evaluation g) Stability study NIPER, Chandigarh

7. Result & discussion a) Particle Morphology F1A Pure LVS F2A NIPER, Chandigarh

8. b) Particle size analysis NIPER, Chandigarh

9. c) Crystalline state evaluation Powder X-Ray diffraction (PXRD): A A A NIPER, Chandigarh

10. Differential scanning calorimetry (DSC): A Endothermic peak: 174.57˚C A Endothermic peak: 174.87˚C A Endothermic peak: 173.92˚C Endothermic peak: 175.19˚C NIPER, Chandigarh

11. d) Solubility determination NIPER, Chandigarh

12. e) In- vitro release studies NIPER, Chandigarh

13. f) In- vivo evaluation In vivo drug release of pure LVS In vivo drug release of F1A and F2A nanocrystals NIPER, Chandigarh

14. Comparison of Bioavailability of LVS nanocrystals * Time in minute Values of Cmax are mean ± standard deviation NIPER, Chandigarh

15. g) Stability study Drug content after 30 days storage of F1A NIPER, Chandigarh

16. Continued….. • Release study of F1A stored at 40C, at 300C±20C / 65%± 5% RH and • at 400C±20C/ 65%± 5% RH NIPER, Chandigarh

17. Conclusion • From the particle morphology by SEM, it was observed that LVS nanocrystals remain crystalline. • Less particle size was observed in case of F1A & F2A as compared to all other. • From PXRD and DSC data, it was observed that F1A , F2A & F3A showed no significant change in crystalline as compared to pure LVS. • Solubility was enhanced due to less particle size & solvent used (acetone & methanol). NIPER, Chandigarh

18. Conclusion • In-vitrorelease rate studies showed that the maximum drug release was found in the F1A & F2A in the required period of time. • In-vivorelativebioavailability of F1A & F2A was slightly increased as compared to absolute bioavailability. • From stability study data it was revealed that nanocrystals of lovastatin remained more stable at 4ºC. The maximum instability of nanocrystals was observed at 402C. NIPER, Chandigarh

19. THANK YOU…. THANK YOU E-mail: bknanjwade@yahoo.co.in Cell No: 0091974243100 NIPER, Chandigarh