Use of Nanohybrid Material for Formulation, Development and Evaluation of Pharmaceutical Dosage Form Containing the Low Solubility Active Pharmaceutical Ingredient
In oral absorption of a drug, the drug first dissolves and then is absorbed by diffusion through gastrointestinal membranes. The gastrointestinal environment is aqueous in nature and it is well-known that one-third of the drug population is water insoluble. Hence, there is a need for enhancement of the solubility and dissolution of such drugs. In this work, enhancement of the solubility and dissolution of the practically insoluble drug Rosuvastatin Calcium was achieved by formation of nanohybrids using microwave-induced diffusion (MIND), which ultimately leads to bioavailability enhancement. nanohybrids were formed by using natural carriers such as acacia,guar gum and PVP k-30 with the help of microwaves. Selection of carriers was based on their surfactant and wetting properties. Solubility studies were carried out to establish the solubility-enhancing property of the nanohybrids. To support solubility analysis results, dissolution studies (i.e. powder dissolution and in-vitro dissolution) were carried out. The nanohybrids were characterized by Fourier transform infrared spectroscopy, differential scanning calorimetry, X-ray diffraction studies, scanning electron microscopy and transmission electron microscopy. It was found that as the concentration of polymer in the composite increased the solubility and dissolution of rosuvastatin calcium were enhanced. The optimised ratio (drug : polymer) for all the composites was found to be 1:4. The novelty of this work is the green and cost-effective way of forming drug nanocomposites with the help of microwave, which can be scaled up to an industrial level. The method gives an immaculate means of solubilisation by generating drug dispersion at the micro and nanoscale level in natural biodegradable stabilising media. Hence, this study demonstrates the use of nanohybrids in solubility and dissolution enhancement.
Keywords- BCS Class II, Nanohybrids, Solubilization, Enhancement of solubility, Optimized drug dissolution and drug release.
2. Bergese P et al. Microwave generated nanocomposites for making insoluble drugs soluble. Mater Sci Eng C 2003, 6–8: 791–795
3. Dash V, Kesari A. Role of biopharmaceutical classification system in drug development program; Journal of Current Pharmaceutical Research; 2011; 5 (1): 28-31
4. Waterbeemd H. V. and Testa B. Drug bioavailability: Estimation of solubility, permeability, absorption and bioavailability, 2nd ed., Wiley-VCH publisher, Weinheim2009
5. Savjani KT, Anuradha KG, Jignasa KS. Drug Solubility: Importance and Enhancement Technique, International Scholarly Research Network, 2012
6. Lachman L, Lieberman HA , Kanig JK. The Theory And Practise of Industrial Pharmacy, Lea & Febiger, 3rd edition, 1986.
7. Martin A, Solubility and Distribution Phenomena, Physical Pharmacy and Pharmaceutical Sciences, Lippincott Williams and Wilkins, 6th edition, 2011
8. Aulton M, “Dissolution and solubility,” in Pharmaceutics: The Science of Dosage form Design, M. E. Aulton, Ed., p. 15, Churchill Livingstone, 2nd edition, 2002.
9. Sharma D, Soni M, Kumar S, Gupta GD, “Solubility enhancement—eminent role in poorly soluble drugs,” Research Journal of Pharmacy and Technology, vol. 2, no. 2, pp. 220–224, 2009.
10. Amidon GL, Lennernas H, Shah VP, Crison JR, “A ¨ theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability,” Pharmaceutical Research, vol. 12, no. 3, pp. 413–420, 1995.
11. Pandya S, Nanocomposites and its application –A Review, Reasearch Gate
12. Okpala C. Nanocomposites - An Overview, International Journal of Engineering Research and Development. 2013; 8: 17-23.
13. Shchipunov Y. Bionanocomposites: Green sustainable materials for the near future. Pure Appl. Chem. 2012; 84: 2579-2607.
14. Pande VV and Sanklecha VM*, Austin Journal of Nanomedicine & Nanotechnology, Bionanocomposite: A Review
15.Wong, T., Use of microwave in processing of drug delivery systems. Curr Drug Delivery : 2008, 5: 77–84
16. Zhou J, Shi C, Mei B, Yuan R, Fu Z. Research on the technology and the mechanicalproperties of the microwave processing of polymer. J. Mater. Process. Tech.: 2003, 137: 156–158.
17.Kushare, S. S., Gattani S. G., Microwave-generated bionanocomposites for solubility and dissolution enhancement of poorly water-soluble drug glipizide: in-vitro and in-vivo studies in-vitro and in-vivo studies. Journal of pharmacy and pharmacology; 2013, 65, 79-93
18. Darder M, Aranda P, Hitzky E. Bionanocomposites: A New Concept of Ecological, Bioinspired, and Functional Hybrid Materials. Adv. Mater. 2007; 19: 1309-1319.
19. Bonde MN, Sohani AC, Daud AS, Sapkal NP: Microwave: An emerging trend in pharmaceutical processes and formulations; International Journal Of Pharmacy & Technology , Vol. 3 (4), 3499-3520.
20. Bhat MR, Payghan SA, Batra AK , Chimkode RM, Bhandari A, Bionanocomposites: technique towards Enhancement of Solubility, Drug Release and Bioavailability, Journal of Medical and pharmaceutical Innovation. 2015, 6-11
21 .S. A. Papadimitriou , D. Bikiaris, Microwave induced enhancement of the dissolution rate of poorly water soluble Tibolone from poly (ethylene glycol) solid dispersion, J. App. Poly. Sci. 108 ,2008 1249-1258
22. S. M. Choi, H. Awaji, Nanocomposites- a new material design concept, Science and Technology of Advanced Materials. 06 , 2005 2–10.
23. Science Murali Mohan Babu, G.V.; Prasad, Ch. D.S.; Raman Murthy, K.V. Evaluation of modified gum karaya as carrier for the dissolution enhancement of poorly water soluble drug nimodipine. Int. J. Pharm.; , v.234, p.1- 17
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 3.0 Unported License. that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (SeeÂ The Effect of Open Access).