Volume : 12, Issue : 06, June – 2025

Title:

ENHANCEMENT OF SOLUBILITY AND DISSOLUTION RATE OF POORLY WATER-SOLUBLE DRUG BY HYDROTROPIC SOLID DISPERSION

Authors :

Aayush Nitin Kole, Dr Nitin S Bhajipale, Dr Prof Vaishali M Vaidya, Sakshi Anil Kharate

Abstract :

A major obstacle in the development of effective oral drug formulations is the poor aqueous solubility of many active pharmaceutical ingredients (APIs), which directly affects their dissolution rate and bioavailability. This limitation often results in inconsistent therapeutic effects and challenges in achieving optimal clinical outcomes. In recent years, the integration of hydrotropic solubilization with solid dispersion technology has emerged as a promising strategy to address this issue. Hydrotropy involves the use of hydrotropic agents highly water-soluble, non-toxic compounds such as sodium benzoate, urea, or citric acid that significantly enhance the solubility of poorly water-soluble drugs by altering the solvent environment without forming micelles. When these agents are combined with solid dispersion techniques, where the drug is molecularly dispersed in a hydrophilic carrier such as PEG or PVP, the resultant system exhibits improved wettability, reduced particle size, and transformation to an amorphous state each contributing to increased dissolution rates. This study explores the formulation of hydrotropic solid dispersions of a model poorly water-soluble drug, focusing on optimizing the ratio of drug to hydrotrope and polymer, evaluating physicochemical properties, and assessing the improvement in solubility and dissolution behavior through in vitro analysis. The findings suggest a marked enhancement in both solubility and dissolution rate compared to pure drug and conventional solid dispersions, indicating the potential of this novel approach in overcoming solubility-related challenges in drug delivery. This technique offers a scalable, cost-effective, and efficient pathway to improve the bioavailability of poorly soluble drugs, ultimately enhancing therapeutic efficacy and patient compliance.[7][8][9]

Cite This Article:

Please cite this article in press Aayush Nitin Kole al., Enhancement Of Solubility And Dissolution Rate Of Poorly Water-Soluble Drug By Hydrotropic Solid Dispersion, Indo Am. J. P. Sci, 2025; 12(06).

Number of Downloads : 10

References:

1. Zhang X, Xing H, Zhao Y, Ma Z. Pharmaceutical dispersion techniques for dissolution and bioavailability enhancement of poorly water-soluble drugs. Pharmaceutics. 2018;10(4):74.
2. Kesharwani A, Kesharwani A, Maqbool MA, Pathak S, Mishra MK. Solubilization enhancement techniques: an overview. The Pharmaceutical and Chemical Journal. 2017;4(6):121–130.
3. Edward KH, Li D. Solubility. In: Drug-Like Properties: Concepts, Structure Design and Methods from ADME to Toxicity Optimization. Elsevier; p. 56.
4. Lachman L, Lieberman H, Kanig JL. The Theory and Practice of Industrial Pharmacy. 3rd ed. Philadelphia: Lea & Febiger; 1986.
5. Ahmad Z, Maurya N, Mishra K, Khan I. Solubility enhancement of poorly water-soluble drugs: a review. International Journal of Pharmacy and Technology. 2011;2(1):807–823.
6. Sharma D, Soni M, Kumar S, Gupta GD. Solubility enhancement: eminent role in poorly soluble drugs. Research Journal of Pharmacy and Technology. 2009;2(2):220–224.
7. Reddy B, Karunakar A. Biopharmaceutics Classification System: A regulatory approach. Dissolution Technologies. 2011;18(3):31–37.
8. Lindenberg M, Kopp S, Dressman J. Classification of orally administered drugs on the WHO model list of essential medicines according to the Biopharmaceutics Classification System. European Journal of Pharmaceutics and Biopharmaceutics. 2004;58(2):265–278.
9. Pant P, Bansal K, Rama TR, Padhee K, Sathapathy A, Kochhar PS. Micronization: an efficient tool for dissolution enhancement of Dienogest. International Journal of Drug Development & Research. 2011;3(2):329–333.
10. Vishal R, Patel, Agrawal YK. Nanosuspension: An approach to enhance the solubility of drug. J Adv Pharm Technol Res. 2011;2(2):81–87.
11. Maulvi F, Thakkar VT, Soni TG, Gohel MC, Gandhi TR. Supercritical fluid technology: A promising approach to enhance the drug solubility. J Pharm Sci Res. 2009;1(4):1–14.
12. Raza K, Kumar P, Ratan S, Malik R, Arora S. Polymorphism: The phenomenon affecting the performance of drugs. SOJ Pharm Sci. 2014;1(2):1–10.
13. Shinde SS, Patil SS, Mevekari FI, Satpute AS. An approach for solubility enhancement: solid dispersion. Int J Adv Pharm Sci. 2010;1(3):299–308.
14. Chiou WL, Riegelman S. Pharmaceutical applications of solid dispersion system. J Pharm Sci. 1971;60(9):1281–1302.
15. Patidar K, Soni M, Sharma KD, Jain KS. Solid dispersion: approaches, technology involved, unmet need and challenges. Drug Invention Today. 2010;2(7):349–357.
16. Kumar BP, Rao S, Murthy KVR, Sahu RK, Ramu B. Solid dispersion: a tool for enhancing bioavailability of poorly soluble drugs. J Chem Pharm Sci. 2011;4(4):170–179.
17. Arunachalam A, Karthikeyan M, Konam K, Prasad PH, Sethuraman S, Ashutoshkumar S. Solid dispersions: A review. Curr Pharm Res. 2010;1(1):82–90.
18. Kapoor B, Kaur R, Behl H, Kour S. Solid dispersion: an evolutionary approach for solubility enhancement of poorly water soluble drugs. Int J Recent Adv Pharm Res. 2012;2(2):1–16.
19. Bhut VZ, Prajapati AB, Patel KN, Patel BA, Patel PA. Solid dispersion as a strategy to enhance solubility: A review article. Int J Pharm Res Scholars. 2012;3(4):277–283.
20. Dhiman S, Kaur P, Arora S. Solid dispersion: opportunity in drug delivery system. Drug Invention Today. 2012;4(10):478–486.
21. Mehta A, Vasanti S, Tyagi R, Shukla A. Formulation and evaluation of solid dispersion of an anti-diabetic drug. Curr Trends Biotechnol Pharm. 2020;3(1):76–84.
22. Thenesh-Kumar S, Gnana-Prakash D, Nagendra-Gandhi N. Effect of hydrotropes on the solubility and mass transfer coefficient of 2-nitrobenzoic acid. Polym J Chem Technol. 2009;11:54–58.
23. Ramesh N, Jayakumar C, Nagendra-Gandhi N. Effective separation of petro products through hydrotropy. Chem Eng Technol. 2009;32(1):129–133.
24. Rodriguez A, Gracini M, Moya ML. Effects of addition of polar organic solvents on micellization. Langmuir. 2008;24:12.
25. Maheshwari RK, Indurkhya A. Formulation and evaluation of aceclofenac injection made by mixed hydrotropic solubilization technique. Iran J Pharm Res. 2010;9(3):233–242.
26. Kwon GS, Okano T. Polymeric micelles as new drug carriers. Adv Drug Deliv Rev. 1996;21:107–116.
27. Rosler A, Vandermeulen GM, Klok HA. Advanced drug delivery devices via self-assembly of amphiphilic block copolymers. Adv Drug Deliv Rev. 2001;53:95–108.
28. Trubetskoy VS. Polymeric micelles as carriers of diagnostic agents. Adv Drug Deliv Rev. 1999;37:81–88.
29. Kataoka K, Harada A, Nagasaki Y. Block copolymer micelles for drug delivery: design, characterization and biological significance. Adv Drug Deliv Rev. 2001;47:113–131.
30. Ghogare D, Patil S. Hydrotropic solubilization: Tool for eco-friendly analysis. Int J Pharm Pharm Res. 2018;11:300–322.
31. Dhapte V, Mehta P. Advances in hydrotropic solutions: An updated review. St. Petersburg Polytech Univ J Phys Math. 2015;1:424–435.
32. Gawai MN, Aher SS, Saudagar RB. Mixed hydrotropy technique for solubility enhancement – A review. Int J Institutional Pharm Life Sci. 2015:442–452.
33. Husain A, Koshta A, Joshi A, Malviya S, Kharia A. Formulation and evaluation of solid dispersion tablet containing Tinidazole. Int J Pharm Sci Res. 2024;15(4):1223–1237.
34. Pardhi VP, Patel M, Jain K. Formulation development, characterization, and evaluation of bedaquiline fumarate – Soluplus® – solid dispersion. Pharm Dev Technol. 2024;1–12.
35. Alezzy AE, Al-Khedairy EBH. Preparation and evaluation of aceclofenac solid dispersion by fusion technique and effervescent assisted fusion technique: Comparative study. Res J Pharm Technol. 2023;16(11):5358–5365.