Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability
Abstract
The solubility of a solute is the maximum quantity of solute that can dissolve in a certain quantity of solvent or quantity of solution at a specified temperature. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Solubility is essential for the therapeutic effectiveness of the drug, independent of the route of administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. Poorly soluble drugs are often a challenging task for formulators in the industry Conventional approaches for enhancement of solubility have limited applicability, especially when the drugs are poorly soluble simultaneously in aqueous and in non-aqueous media. Drug with poor water solubility cause slow dissolution rates, generally show erratic and incomplete absorption leading to low bioavailability when administered orally. Solubilization may be affected by cosolvent water interaction, micellar solubilization, reduction in particle size, inclusion complexes, solid dispersion, and change in polymorph. Some new technologies are also available to increase the solubility like micro emulsion, self-emulsifying drug delivery system and supercritical fluid technology. This present review details about the different approaches used for the enhancement of the solubility of poorly water-soluble drugs include particle size reduction, nanonization, pH adjustment, solid dispersion, complexation, co‐solvency, hydrotropy etc. The purpose of this article is to describe the techniques of solubilization for the attainment of effective absorption and improved bioavailability.
Keywords: Solubility, Solubility Enhancement, bioavailability, solid dispersion, Solid Dispersion, Solubilization.
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References
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33. Ramesh v., “Enhancement of solubility for poorly water soluble drugs by using solid dsipersion technology”, international journal of pharmaceutical research and bio-science, 2016; 5(2): 47-74, issn: 2277-8713.
34. Singh N, sarangi M. “solid dispersion - A novel approach for enhancement of bioavailability of poorly soluble drugs in oral drug delivery system”. Glob j pharmaceu sci., 2017; 3(2): 555608.doi
35. 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
36. Jaiswal, P., Kesharwani, S., Kesharwani, R., & Patel, D. (2016). Ethosome: a new technology used as topical & transdermal delivery system. Journal of Drug Delivery and Therapeutics, 6(3), 7-17. https://doi.org/10.22270/jddt.v6i3.1245
37. Bhirud, Y., & Phalak, H., Advances in solid dispersion technology and its applications in the development of solid dosage forms. Journal of Drug Delivery and Therapeutics, 2016; 6(6):40-47. https://doi.org/10.22270/jddt.v6i6.1316
38. Hiremath SN, Raghavendra RK (2014) Dissolution enhancement of Gliclazide by preparation of inclusion complexes with β-cyclodextrin. Asian Journal of Pharmaceutics 30: 2057-2060.
39. Enose AA, Dasan P, Sivaramakrishanan H, Kakkar V. Formulation, characterization and pharmacokinetic evaluation of telmisartan solid dispersions. J Mol Pharm Org Process Res 2016;4:1-8
40. UsmanovaLS, ZiganshinMA, GorbatchukV, ZiganshinaSA, BizyaevDA, BukharaevA, et al. A study of the formation of magnetically active solid dispersions of phenacetin using atomic and magnetic force microscopy. J Adv Pharm Tech Res 2017;8:2-7.
41. Duarte I, Corvo ML, Serodio P, Vicente J, Pinto JF, Temtem M, et al. Production of nano-solid dispersions using a novel solvent-controlled precipitation process-Benchmarking their in vivo performance with an amorphous micro-sized solid dispersion produced by spray drying. Eur J Pharm Sci 2016;93:203-214.
42. Sindhu J, Kishore B, Kaza R, Ranganayakulu D. Design and characterization of fast dissolving films of Telmisartan solid dispersions. International journal of research in pharmaceutical and nano sciences. 2015; 4(3):140-52.
43. Begam M, Datta MV, Gowda DV, Aravindaram AS. Development and characterization of co-ground mixtures and solid dispersions of Aripiprazole with hydrophilic carriers. International journal of pharmacy and pharmaceutical sciences. 2014; 6(2):552-57.
44. Haser A, Cao T, Lubach JW, Zhang F. In Situ Salt Formation during Melt Extrusion for Improved Chemical Stability and Dissolution Performance of a Meloxicam– Copovidone Amorphous Solid Dispersion. Molecular pharmaceutics. 2018; 15(3):1226-37.
2. Aulton ME. Pharmaceutics the science of dosage form design. 3rd ed. New York: Churchill Livingstone; 1988: p.25-27.
3. Ali MD. Dictionary of Pharmacy. 2005-06: 357-363.
4. Indian Pharmacopoeia 2007. Ministry of Health and family welfare, Government of India. Published by the controcller of publications, Delhi; 1: p.143, 258, 477.
5. Swarbrick J. Encyclopedia of Pharmaceutical Technology. 3rd ed. New York:Informa healthcare; 2006: p.3314-3328.
6. Rawlins EA. Bentley’s text book of pharmaceutics. 8th ed. Pennsylvania: Sunders Elsevier; 2010: p.5-9, 15-14.
7. Limbachiya MI. Solubility enhancement techniques forpoorly soluble drugs: A review. IJPRD, 2011; 4(4):71-86
8. Patil MS, Godse SG, Saudagar RB. Solubility Enhancement by Various Techniques: An Overview. World Journal of Pharmacy and Pharmaceutical Sciences. 2013; 2(6):4558-4572.
9. Pawar AR, Choudhari PD. Novel Techniques for Solubility, Dissolution Rate and Bioavailability Enhancement of Class II & IV drugs. Asian Journal of Biomedical & Pharmaceutical Science.2012; 13:9-14.
10. Godse SZ, Patil MS, Kothavade SM, Saudagar RB.Techniques for Solubility Enhancement of Hydrophobic Drugs: A Review, J Adv. Pharm. Edu. & Res. 2013; 3(4):403-414.
11. Vemula VR, Lagishetty V, Lingala S. Solubility enhancement techniques, International Journal of Pharmaceutical Sciences Review and Research. 2010; 5(1):41-51.
12. Savjani KT, Gajjar AK, Savjani JS. Drug Solubility: Importance and Enhancement Techniques. ISRN Pharmaceutics Article ID195727, 2012, 1-10, doi:10.5402/2012/195727.
13. N. Blagden, M. de Matas, P.T. Gavan, P. York. Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates, Advanced Drug Delivery Reviews, 2007; 59(7):617-630.
14. M. Vogt, K. Kunath, J.B. Dressman. Dissolution enhancement of fenofibrate by micronization, cogrinding and spray-drying: comparison with commercialpreparations, European Journal of Pharmaceutics and Biopharmaceutics. 2008; 68(2):283-288.
15. Devil NKD, Rani AP, Javed M, Kumar KS, Kaushik J, Sowjanya. Cyclodextrins in pharmacy-An overview, Pharmacophore, 2010; 1(3):155-165.
16. Prabhakar Ch, Bala Krishna K. A Review on Nanosuspensions in Drug Delivery, International Journal Pharma and Bio Sciences. 2011; 2(1):549- 558.
17. Patel M, Shah A, Dr. Patel NM, Dr. Patel MR, Patel Dr. KR. Nanosuspension: A Novel Approach for Drug Delivery System, Journal of Pharmaceutical Science and Bioscintic Res. 2011; 1(1):1-10.
18. Shinde A. Solublization of poorly water soluble drugs: A review. Pharminfo.net 2007; 5(6):1-9.
19. Meera C, Singh AB, Sayyad, Sawant SD. Review on various techniques of solubility enhancement of poorly soluble drugs with special emphasis on solid dispersion. J Pharmacy Res. 2010; 3(10):2494-2501
20. Junghanns JA, Müller RH. Nanocrystal technology, drug delivery and clinical applications. Inter J Nanomedicine 2008; 3(3):295–309.
21. Chiou W, Rieglmans S. Pharmaceutical application of solid dispersion system. J Pharm Sci. 1971; 60(9):1281-1302.
22. Fahr A, Xianglilu. Drug delivery strategies for poorly water soluble drug.Informa healthcare 2007; 4(4):403-416.
23. Kushwaha A. Solid dispersion a promising novel approach for improving the solubility of poorly soluble drugs. Inter J Pharm Sci Res. 2011; 2(8):2021-2030.
24. WadkeDA, Serajuddin A, Jacobson H, “Preformulation testing”. In: Lieberman HA, Lachman L, Schwartz JB, eds. Pharmaceutical Dosage Forms: Tablets. New York, NY: Marcel Dekker; 1989.
25. Brahmankar DM, Jaiswal SB. Biopharmaceutics and Pharmacokinetics, Vallabh Prakashan, 1st Edn.1995:347-352.
26. Patel PB, Prajapati ST, Patel NR, Patel NN, Patel CN. Solid Dispersion: A Method of Improving Bioavailability and Taste Masking. Inventi Rapid: Pharm Tech Vol. 2012; Issue 4.
27. Dhirendra K, Lewis S, Udupa N, Atin K. Solid Dispersion: A Review. Pak. J. Pharm,April 2009;Vol.22(2):234-246.
28. Sambath L, Kottai Muthu A, Ashis Kumar M, et al. Formulation and evaluations of Naproxen sustained release tablets using Naproxen solid dispersion. Inventi Rapid: Pharm Tech 2013.
29. Gattani S, Moon R. Formulation and in vitro evaluation of tablet containing gliclazide nanocrystals for solubility and dissolution enhancement using Soluplus. IJPSR. 2018; 9(1):133-139.
30. Pandey MM, Kumar GK, Ramakrishan R, Chardet S. Solubility enhancement of felodipine by solid dispersions with novel polymeric solubilizer Soluplus. J. Bioequi. Availab. 2012; 4(3):146.
31. Sultan sakina and safiuddin. ahm. “review article: solid dispersion currently practiced in pharmaceutical field” international journal of advancements in research & technology, march-2016; 5(3): 2278-7763.
32. Younis a. Mahmoud, “solid dispersion technology, a contemporary overview on a well established technique”, universal journal of pharmaceutical research, 2017; 2(3): 2456-8058.
33. Ramesh v., “Enhancement of solubility for poorly water soluble drugs by using solid dsipersion technology”, international journal of pharmaceutical research and bio-science, 2016; 5(2): 47-74, issn: 2277-8713.
34. Singh N, sarangi M. “solid dispersion - A novel approach for enhancement of bioavailability of poorly soluble drugs in oral drug delivery system”. Glob j pharmaceu sci., 2017; 3(2): 555608.doi
35. 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
36. Jaiswal, P., Kesharwani, S., Kesharwani, R., & Patel, D. (2016). Ethosome: a new technology used as topical & transdermal delivery system. Journal of Drug Delivery and Therapeutics, 6(3), 7-17. https://doi.org/10.22270/jddt.v6i3.1245
37. Bhirud, Y., & Phalak, H., Advances in solid dispersion technology and its applications in the development of solid dosage forms. Journal of Drug Delivery and Therapeutics, 2016; 6(6):40-47. https://doi.org/10.22270/jddt.v6i6.1316
38. Hiremath SN, Raghavendra RK (2014) Dissolution enhancement of Gliclazide by preparation of inclusion complexes with β-cyclodextrin. Asian Journal of Pharmaceutics 30: 2057-2060.
39. Enose AA, Dasan P, Sivaramakrishanan H, Kakkar V. Formulation, characterization and pharmacokinetic evaluation of telmisartan solid dispersions. J Mol Pharm Org Process Res 2016;4:1-8
40. UsmanovaLS, ZiganshinMA, GorbatchukV, ZiganshinaSA, BizyaevDA, BukharaevA, et al. A study of the formation of magnetically active solid dispersions of phenacetin using atomic and magnetic force microscopy. J Adv Pharm Tech Res 2017;8:2-7.
41. Duarte I, Corvo ML, Serodio P, Vicente J, Pinto JF, Temtem M, et al. Production of nano-solid dispersions using a novel solvent-controlled precipitation process-Benchmarking their in vivo performance with an amorphous micro-sized solid dispersion produced by spray drying. Eur J Pharm Sci 2016;93:203-214.
42. Sindhu J, Kishore B, Kaza R, Ranganayakulu D. Design and characterization of fast dissolving films of Telmisartan solid dispersions. International journal of research in pharmaceutical and nano sciences. 2015; 4(3):140-52.
43. Begam M, Datta MV, Gowda DV, Aravindaram AS. Development and characterization of co-ground mixtures and solid dispersions of Aripiprazole with hydrophilic carriers. International journal of pharmacy and pharmaceutical sciences. 2014; 6(2):552-57.
44. Haser A, Cao T, Lubach JW, Zhang F. In Situ Salt Formation during Melt Extrusion for Improved Chemical Stability and Dissolution Performance of a Meloxicam– Copovidone Amorphous Solid Dispersion. Molecular pharmaceutics. 2018; 15(3):1226-37.
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Pawar SR, Barhate SD. Solubility enhancement (Solid Dispersions) novel boon to increase bioavailability. JDDT [Internet]. 22Mar.2019 [cited 18Apr.2024];9(2):583-90. Available from: https://www.jddtonline.info/index.php/jddt/article/view/2437
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