• P.v. S. S. Sanjaymitra Department of Pharmaceutical Sciences, JSS College of Pharmacy, Udhagamandalam, TamilNadu, pin 643001
  • G. N. K. Ganesh Department of Pharmaceutical Sciences, JSS College of Pharmacy, Udhagamandalam, TamilNadu, pin 643001


The solubility is one of the important parameters to achieve the desired concentration of the drug in the systemic circulation in pharmacological response to be shown. The oral route is the most desirable and preferred method of administering therapeutic agents for their systemic effects, but the poor solubility of the drug is a major challenge for formulation scientist. Close to 40% of orally administered drugs suffer from formulation difficulties related to their water insolubility. Dissolution rate, absorption, distribution, and excretion of a moiety depend upon its solubility characteristics. Although several advantages associated with the oral route, the poorly soluble drugs suffer from slow dissolution and poor bioavailability. Based on solubility, drugs are classified into four classes of the BCS classification. Solubility challenges are faced in ClassII and Class IV of the BCS system this is important because most of the generic and NCE drugs come under class II drugs. The solubility behavior of drugs remains one of the most challenging aspects of formulation development. There are several methods available for solubility and dissolution enhancement of poorly water-soluble drugs. The aim of this clause is to distinguish the techniques of solubilization for the acquisition of effective absorption and improved bioavailability.

Keywords: Solubility, Biopharmaceutical classification (BCS), pH, Dissolution


1. Sikarra D, Shukla VA, Kharia AA, Chatterjee DP. Techniques for solubility enhancement of poorly soluble drugs: an overview. J Med Pharm Allied Sci 2012;1:1-22.
2. Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN Pharmaceutics 2012. http://dx.doi.org/10.5402/2012/195727
3. Kadam SV, Shinkar DM, Saudagar RB. Review of solubility enhancement techniques. Int J Pharma Bio Sci 2013;3:462-75.
4. Patel A. Solubility enhancement technologies and research emerged. Int J Pharma Biol Arch 2017;8:1-11 .
5. Kumar S, Singh P. Various techniques for solubility enhancement: an overview. Pharma Innov J 2016;5:23-8.
6. Vasconcelos T, Sarmento B, Costa P. Solubility enhancement as strategies to improve oral bioavailability of poorly water-soluble drugs. Drug Discovery Today 2007;12:1281-302.
7. Behera AL, Sahoo SK, Patil SV. Enhancement of solubility: a pharmaceutical overview. Der Pharm Lett 2010;2:310-8.
8. Patel RP, Baria AH, Patel NA. An overview of size reduction technologies in the field of pharmaceutical manufacturing. Asian J Pharm 2014;2:216-20.
9. Rasenack N, Müller BW. Micron‐size drug particles: common and novel micronization techniques. Pharm Dev Technol 2004;9:1-3.
10. Vandana KR, Raju YP, Chowdary VH, Sushma M, Kumar NV. An overview of in situ micronization technique–An emerging novel concept in advanced drug delivery. Saudi Pharma J 2014;22:283-9.
11. Vogt M, Kunath K, Dressman JB. Dissolution enhancement of fenofibrate by micronization, cogrinding, and spray-drying: comparison with commercial preparations. Eur J Pharm Biopharm 2008;68:283-8.
12. Junyaprasert VB, Morakul B. Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs. J Pharm Sci 2015;10:13-23.
13. Budiman A, Nurlatifah E, Amin S. Enhancement of solubility and dissolution rate of glibenclamide by cocrystal approach with solvent drop grinding method. Int J Curr Pharm Rev Res 2016;7:248-50.
14. Hickey MB, Peterson ML, Scoppettuolo LA, Morrisette SL, Vetter A, Guzman H, et al. Performance comparison of a co-crystal of carbamazepine with a marketed product. Eur J Pharm Biopharm 2007;67:112-9.
15. Iyan Sopyan, Achmad Fudholi, Muchtaridi, Ika Puspitasari. A simple effort to enhance solubility and dissolution rate of simvastatin using co-crystalization. Int J Pharm Pharm Sci 2016;8:342-6.
16. Breitenbach J. Melt extrusion: from process to drug delivery technology. Eur J Pharm Biopharm 2002;54:107-17.
17. Sugimoto S, Niwa T, Nakanishi Y, Danjo K. Novel ultra-cryo milling and co-grinding technique in liquid nitrogen to produce dissolution-enhanced nanoparticles for poorly water-soluble drugs. Chem Pharm Bull 2012;60:325-33.
18. Junghanns JU, Müller RH. Nanocrystal technology, drug delivery, and clinical applications. Int J Nanomed 2008;3:295.
19. Palani KA, Kesavan SK. Enhancement of rosuvastatin calcium bioavailability applying nanocrystal technology and in vitro, in vivo evaluations. Asian J Pharm Clin Res 2015;8:88-92.
20. Junyaprasert VB, Morakul B. Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs. Asian J Pharm Sci 2015;10:13-23.
21. Peltonen L, Hirvonen J. Pharmaceutical nanocrystals by nano milling: critical process parameters, particle fracturing, and stabilization methods. J Pharm Pharmacol 2010;62:1569-79.
22. Junyaprasert VB, Morakul B. Nanocrystals for enhancement of oral bioavailability of poorly water-soluble drugs. Asian J Pharm Sci 2015;10:13-23.
23. Spireas SS, Jarowski CI, Rohera BD. Powdered solution technology: principles and mechanism. Pharm Res 1992;9:1351-8.
24. Lu M, Xing H, Jiang J, Chen X, Yang T, Wang D, et al. Liquisolid technique and its applications in pharmaceutics. Asian J Pharm Sci 2017;12:115-23.
25. Khames A. Investigation of the effect of solubility increases at the main absorption site on the bioavailability of BCS class II drug (risperidone) using a liquisolid technique. Drug Delivery 2017;24:328-38.
26. Satyajit Panda, R Varaprasad, K Priyanka, Ranjit P Swain. Liquisolid technique: a novel approach for dosage form design. Int J Appl Pharm 2017;9:8-14.
27. Tiong N, Elkordy AA. Effect of liquisolid formulations on the dissolution of naproxen. Eur J Pharm Biopharm 2009;73:373–84.
28. Javaheri H, Carter P, Elkordy A. Wet granulation to overcome liquisolid technique issues of poor flowability and compatibility: a study to enhance glibenclamide dissolution. J Pharm Drug Dev 2014;1:501-12.
29. Javadzadeh Y, Siahi-Shadbad MR, Barzegar-Jalali M, Nokhodchi A. Enhancement of dissolution rates of piroxicam using liquisolid compacts. IL Farmaco 2005;60:361-5.
30. Talari R, Nokhodchi A, Mostafavi SA, Varshosaz J. Dissolution enhancement of Gliclazide using the pH change approach in the presence of twelve stabilizers with various physicochemical properties. J Pharm Pharm Sci 2009;12:250-65.
31. Humayun HY, Shaarani MN, Abdullah B, Salam MA. The effect of Co-solvent on the solubility of a sparingly soluble crystal of benzoic acid. Procedia Eng 2016;148:1320-5.
32. Khan MA. Novel application of mixed solvency concept using poorly water-soluble drug diclofenac sodium. Int J Res Pharm Chem 2012;2:1040-2.
33. Hsu CH, Cui Z, Mumper RJ, Jay M. Micellar solubilization of some poorly soluble antidiabetic drugs. AAPS PharmSciTech 2008;9:939-43.
34. Muzaffar FA, Singh UK, Chauhan LA. Review on microemulsion as futuristic drug delivery. Int J Pharm Pharma Sci 2013;5:39-53.
35. Jha SK, Dey S, Karki S. Microemulsions-potential carrier for improved drug delivery. Asian J Biomed Pharm Sci 2011;1:5-9 .
36. Singh V, Bushettii SS, Raju AS, Ahmad R, Singh M, Bisht A. Microemulsions as promising delivery systems: a review. Indian J Pharm Edu Res 2011;45:392-401.
37. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-micro emulsifying’drug delivery systems. Eur J Pharm Sci 2000;11:S93-8.
38. Sercombe L, Veerati T, Moheimani F, Wu SY, Sood AK, Hua S. Advances and challenges of liposome assisted drug delivery. Front Pharmacol 2015;6:286.
39. Akbarzadeh A, Rezaei-Sadabady R, Davaran S, Joo SW, Zarghami N, Hanifehpour Y, et al. Liposome: classification, preparation, and applications. Nanoscale Res Lett 2013;8:102.
40. Hussain A, Rytting JH. Prodrug approach to enhancement of the rate of dissolution of allopurinol. J Pharm Sci 1974;63:798-9.
41. Yadav AV, Shete AS, Dabke AP, Kulkarni PV, Sakhare SS. Co-crystals: a novel approach to modify physicochemical properties of active pharmaceutical ingredients. Indian J Pharm Sci 2009;71:359.
42. Manish M, Harshal J, Anant P. Melt sonocrystallization of ibuprofen: effect on crystal properties. Eur J Pharm Sci 2005;25:41-8.
43. Gogate PR, Tayal RK, Pandit AB. Cavitation: a technology on the horizon. Curr Sci 2006;91:35-46.
44. Rajanikant P, Nirav P, Patel NM, Patel MM. A novel approach for the dissolution enhancement of Ibuprofen by preparing floating granules. Int J Res Pharm Sci 2016;1:57-64.
45. Khadka P, Ro J, Kim H, Kim I, Kim JT, Kim H, et al. Pharmaceutical particle technologies: an approach to improve drug solubility, dissolution, and bioavailability. Asian J Pharm Sci 2014;9:304-16.
46. Naseem A, Olliff CJ, Martini LG, Lloyd AW. Effects of plasma irradiation on the wettability and dissolution of compacts of griseofulvin. Int J Pharm 2004;269:443-50.
47. Huang ZM, Zhang YZ, Kotaki M, Ramakrishna S. A review on polymer nanofibers by electrospinning and their applications in nanocomposites. Compos Sci Technol 2003;63:2223-53.
48. Löbmann K, Svagan AJ. Cellulose nanofibers as excipient for the delivery of poorly soluble drugs. Int J Pharm 2017;533:285-97.
49. Pawar AP, Paradkar AR, Kadam SS, Mahadik KR. Crystallo-co-agglomeration: a novel technique to obtain ibuprofen-paracetamol agglomerates. AAPS PharmSciTech 2004;5:57-64.
50. Rogers TL, Hu J, Yu Z, Johnston KP, Williams RO. A novel particle engineering technology: spray-freezing into liquid. Int J Pharm 2002;242:93-100.
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How to Cite
Sanjaymitra, P. S. S., & Ganesh, G. N. K. (2018). DISSOLUTION AND SOLUBILITY ENHANCEMENT STRATEGIES: CURRENT and NOVEL PROSPECTIVES. Journal of Critical Reviews, 5(3), 1-10. https://doi.org/10.22159/jcr.2018v5i3.23451
Pharmaceutical Sciences