Chemical Modification: A unique solutions to Solubility problem
Almost 40% of the new chemical entities at present self find out poorly water soluble drugs. Badly water soluble drugs have solubility and dissolution related bioavailability problems. Solubility is one of the most important parameter to give desired concentration of drug in systemic circulation to get its pharmacological response. Orally administered drugs obtained completely absorb only when they show fair solubility in gastric medium and such drugs shows good bioavailability. The solubility and dissolution properties of drugs perform an valuable role in the process of formulation development. Enhancement of solubility of drug is the most challenging job in drug development process. Solubilization may be affected by co solvent water interaction, micellar solubilization, reduction in particle size, inclusion complexes, solid dispersion, and change in polymorph. This review highlight various techniques of solubility enhancement with special emphasis on Chemical modification methods like Salt formation, Co-crystallization, Co-solvency, Hydrotropy, use of novel solubilizer etc along with physical modification techniques.
Keywords: Salt formation, Co-crystallization, Solubility, particle technologies, Milling solubility enhancement, Cosolvent, physical and chemical methods.
2. Dhobale AV, Dhembre GN, Shaikh KU, Shaikh IA, Nandkishor B. Bavage, Kulkarni A. solubility enhancement techniquesa review. IAJPS 2018, 05 (04), 2798-2810.
3. Kumar S, Singh P, Various techniques for solubility enhancement: An overview. The Pharma Innovation Journal 2016; 5(1):23-28.
4. Mankar SD, Rachh PR, solubility enhancement of poor water soluble drugs by solid dispersion: a review. Journal of Drug Delivery & Therapeutics. 2018; 8(5):44-49. https://doi.org/10.22270/jddt.v8i5.1887
5. Gupta S, Sawarkar S, Ravikumar P, “ solubility enhancement of poorly water soluble protease inhibitor” international journal of pharmacuitical sciences and research, 2016; 7(1):252-258.
6. Deepak G, Wage S.R, Suresh Bora, Priyanka D Swati deore , Datta magar, “solubility enhancement of nepafenac solubilizers” european journal of pharmaceutical and medical research 2016; 2(3):181-185.
7. Rajaiya P, Mishra R, Nandgude T, Poddar SK, “ solubility and dissolution enhancement of albendazole by spherical crystallization” published on: 23/01/2016, research article, Asian journal of biomedical and pharmaceutical sciences, 2016; 1-16.
8. Shah NV, Seth AK, Balaraman C. Rajesha J, Maheshwari A, Parmar GR, “nanostructured lipid carriers for oral bioavailability enhancement of raloxifene design and in vivo study” journal of advanced research, accepted manuscript, 2016; 1-34.
9. Zoghbi A., Wang B., Carvedilol solubility enhancement by inclusion complexation and solid dispersion: review. Journal of Drug Delivery and Therapeutics, 2015; 5(2):1-8. https://doi.org/10.22270/jddt.v5i2.1074
10. Ganesan P, Soundararajan R, Shanmugam U, Ramu R, original research paper development, “characterization and solubilityenhancement of comparative dissolution study of second generation of solid dispersions andmicrospheres for poorly water soluble drug” asian journal of pharmaceutical sciences, 2015; 10:433-441.
11. Shah D., Patel B., & Shah C.,. Nanosuspension technology: A innovative slant for drug delivery system and permeability enhancer for poorly water soluble drugs. Journal of Drug Delivery and Therapeutics, 2015; 5(1):10-23. https://doi.org/10.22270/jddt.v5i1.995
12. Kannao SU , Bakade BV, “solid dispersion technique for solubility enhancement of weakly water soluble drug” world journal of pharmaceutical research, 2015; 5(1):1242-1254
13. Khadka P, jieu RO, Kim H, Kim I, Kim JT, Kim H, Cho JM et al “pharmaceutical particle technologies: an approach to improve drug solubility, dissolution andbioavailability” asian journal of pharmaceutical sciences, 2014; 304-316.
14. Pande S.V, Biyan K.R, “solid dispersion: an effective approach for bioavailability enhancement for poorly soluble drugs” american journal of pharmtech research 2014; 2(7):0-57.
15. Kadam SV, Shinkar DM, Saudagar RB, “review on solubility enhancement techniques” international journal of pharmacy and biological sciences, 2013; 3(3):462-575.
16. Purushottam B. Malode, nikhilesh P. Karandikar, Avinash B. Darekar, ravindra b.saudagar, “newer techniques to enhance the bioavailability of hydrophobicdrugs by means of solubility enhancement: a review” american journal of pharmtech research, accepted 09 december 2013; 4(1):77-95.
17. Kushwaha AK, vuddanda PR, Karunanidhi P, Singh SK and Singh S. “development and evaluation of solid lipid nanoparticles of raloxifene hydrochloride for enhanced bioavailability” biomed research international, 2013; 1-9.
18. Gong j. Chen, m. Zheng y, wang s. And wang y. “polymeric micelles drug delivery system in oncology. J. Control. Release” 2012; 312–323.
19. Shariare MH, blagden N and Matas MD, “influence of solvent on the morphology and subsequent comminutionof ibuprofen crystals by air jet milling” journal of pharmaceutical science, 2012; 1108-1119.
20. Gong j. Chen, M. Zheng Y, Wang S, nd Wang Y. “polymeric micelles drug delivery system in oncology. J. Control. Release” 2012, :. 312–323.
21. Shariare MH, Blagden N And Matas MD, “influence of solvent on the morphology and subsequent comminutionof ibuprofen crystals by air jet milling” journal of pharmaceutical science,2012; 1108-1119.
22. Bilgili E And Afolabi A, “a combined microhydrodynamicspolymeradsorption analysis for elucidation of the roles of stabilizers in wet stirred media milling” international journal of pharmacy, 2012; 193-206.
23. Ghosh I, Schenck D, And Bose S, “optimization of formulation and process parameters for the production of Nanosuspension by wet media milling technique and effect of vitamin tpgs, nanocrystal particle size on oral absorption” european journal of pharmaceutical science, 2012, :.718-728.
24. Anhalt K, geissler S, harms M, “development of a new to assess nanocrystal dissolution based on light Scattering” pharma reserarch 2012; 2887-2901.
25. De Smet L, Colin P And Ceelen W, “development of a nanocrystalline paclitaxel formulation for hipec treatment” pharm research 2012; 2398-2406.
26. Bose S, Schenck D, Ghosh I, “application of spray granulation for conversion of a nanosuspension into a dry powder form, european journal of pharmaceutical science, 2012; 35-43.
27. Otte A and carvajal MT. “assessment of milling-induced disorder of two pharmaceutical compounds” j pharm science 2011; 1793-1804.
28. Ghosh I, Bose S, Vippagunta R, “nanosuspension for improving the bioavailability of a poorly soluble drug and screening of stabilizing agents to inhibit crystal growth” international journal pharmacy, 2011; 260-268.
29. Vemula VR, Lagishetty V, Lingala S, “solubility enhancement techniques” international journal of pharmaceutical sciences review and research, 2010; 5(1):42-51.
30. Kataoka K. “development of polymer-based nanodevices for pinpoint therapy and diagnostics” advanced polymers for nanobiotechnology 2009; 58(1).
31. Jagtap S, Magdum C, Jadge D, Jagtap R,Solubility Enhancement Technique: A Review J. Pharm. Sci. & Res., 2018; 10(9):220 -2211
32. Shaikh Siraj N,G. Khan J, Fakir H S, Shaikh Mohsin F, Drug - Drug Solid Dispersion: A Unique Approach In Solubility Enhancement. International Journal of Pharma Research & Review, 2016: 5(1):19-27.
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 4.0 International (CC BY-NC 4.0). 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 (See The Effect of Open Access).