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Author(s): Ms. Aishwarya Audumbar Karande1, Mr. Amol Sampat Deshmukh2

Email(s): 1aishwaryakarande742@gmail.com

Address:

    Department of Pharmaceutics, S.M.B.T. College of Pharmacy, Dhamangaon, Nashik, Maharashtra, India.

Published In:   Volume - 2,      Issue - 2,     Year - 2023

DOI: Not Available

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ABSTRACT:
The phenomenon of a solid dissolving into a liquid phase to create a homogeneous system is known as solubility. To acquire the required concentration of medication in the systemic circulation for the best pharmacological response solubility is a crucial factor. The main issue in developing formulations for new chemical compounds as well as for generic development is low water solubility. About 40% of all newly discovered chemical compounds are lipophilic, which prevents their use in therapeutic doses because of their poor water solubility. Solid dispersion, solvent deposition, micronization, and complexation are a few vital techniques frequently used to improve the solubility of medications that aren't very soluble in water. Poorly water soluble in pharmaceuticals their solubility increased by the use of complexation technology. Such cyclodextrin can interact with appropriate size drug molecules which lead to the formulation of inclusion complexes. In this review, brief information about improvement of aqueous solubility of drug and improve therapeutic efficacy by inclusion complexation method. The solubility, dissolution rate, and bioavailability of poorly soluble pharmaceuticals have been reported to be improved through complexation with CDs using a variety of techniques, including physical mixing, melting, kneading, spray drying, freeze drying, and co-evaporation.

Cite this article:
Ms. Aishwarya Audumbar Karande, Mr. Amol Sampat Deshmukh. Review on Inclusion Complexation: A Technique to Enhance the Solubility of Poorly Water Soluble Drug. IJRPAS, 2023; 2(2): 44-63


1.              Mahale VG, Deshmukh AS, Mahajan VR. Formulation and Characterization of Inclusion Complexes : A Review. 2014;3(3):476–80. 

2.              Kreider GN. A Literary Endorser. J Am Med Assoc. 1897;XXIX(2):90. 

3.              Stegemann S, Leveiller F, Franchi D, de Jong H, Lindén H. When poor solubility becomes an issue: From early stage to proof of concept. Eur J Pharm Sci. 2007 Aug;31(5):249–61. 

4.              Savjani KT, Gajjar AK, Savjani JK. Drug solubility: importance and enhancement techniques. ISRN Pharm. 2012 Jul;2012:1–10. 

5.              Sivakumar M, Tang SY, Tan KW. Cavitation technology – A greener processing technique for the generation of pharmaceutical nanoemulsions. Ultrason Sonochem. 2014 Nov;21(6):2069–83. 

6.                  Morales JO, Watts AB, McConville JT. Mechanical particle-size reduction techniques. AAPS Adv Pharm Sci Ser. 2016 Dec;22:165–213. 

7.                  Merisko-Liversidge E, Liversidge GG, Cooper ER. Nanosizing: a formulation approach for poorly-water-soluble compounds. Eur J Pharm Sci. 2003 Feb;18(2):113–20. 

8.                  Recharla N, Riaz M, Ko S, Park S. Novel technologies to enhance solubility of foodderived bioactive compounds : A review. J Funct Foods [Internet]. 2017;39:63–73. Available from: https://doi.org/10.1016/j.jff.2017.10.001

9.                  Habib, M.J., Pharmaceutical solid dispersion Technology, Technomic Publishing Company, Inc. Lancaster, Pennsylvania (U.S.A.). 2001, pp. 1-36. 

10.              Agarwal A, Singh BK, Trivedi N, Jha KK. Approaches for enhancement of solubility to improve the absorption and bioavailability of poorly soluble drugs. Russ J Biopharm. 2015;7(2):3–8. 

11.              Leuenberger H, Lanz M. Pharmaceutical powder technology — from art to science:

the challenge of the FDA’s Process Analytical Technology initiative. Adv Powder Technol. 2005 Jan;16(1):3–25. 

12.              Davé RN, Bilgili E, Cuitino A, Jallo L. Special issue on pharmaceutical powders: Towards developing understanding of the influence of materials and processes on product performance. Powder Technol. 2013 Feb;236:1–4. 

13.              Dressman JB, Vertzoni M, Goumas K, Reppas C. Estimating drug solubility in the gastrointestinal tract. Adv Drug Deliv Rev. 2007 Jul;59(7):591–602. 

14.              Khadka P, Ro J, Kim H, Kim I, Tae J, Kim H, et al. ScienceDirect Pharmaceutical particle technologies : An approach to improve drug solubility , dissolution and bioavailability. Asian J Pharm Sci [Internet]. 2014;9(6):304–16. Available from: http://dx.doi.org/10.1016/j.ajps.2014.05.005

15.              Soliman OAE, Kimura K, Hirayama F, Uekama K, El-Sabbagh HM, El-Gawad AEGHA, et al. Amorphous spironolactone-hydroxypropylated cyclodextrin complexes with superior dissolution and oral bioavailability. Int J Pharm. 1997 Apr;149(1):73–83. 

16.              Rao VM, Stella VJ. When can cyclodextrins be considered for solubilization purposes? J Pharm Sci. 2003 May;92(5):927–32. 

17.              Tinwalla AY, Hoesterey BL, Xiang T xiang, Lim K, Anderson BD. Solubilization of thiazolobenzimidazole using a combination of pH adjustment and complexation with 2-hydroxypropyl-beta-cyclodextrin. Pharm Res. 1993;10(8):1136–43. 

18.              Szejtli J. Medicinal applications of cyclodextrins. Med Res Rev. 1994;14(3):353–86. 

19.              Tetsumi I, Yoshinobu T, Kaneto U, Pitha J. Effect of bile on the intestinal absorption of α-cyclodextrin in rats. Int J Pharm. 1988 Apr;43(1–2):41–4. 

20.              Hirayama F, Uekama K. Cyclodextrin-based controlled drug release system. Adv Drug Deliv Rev. 1999 Mar;36(1):125–41. 

21.              Loftsson T, Brewster ME. Pharmaceutical applications of cyclodextrins. 1. Drug solubilization and stabilization. J Pharm Sci. 1996;85(10):1017–25. 

22.              Stella VJ, Rao VM, Zannou EA, Zia V. Mechanisms of drug release from cyclodextrin complexes. Adv Drug Deliv Rev. 1999 Mar;36(1):3–16. 

23.              Carrier RL, Miller LA, Ahmed I. The utility of cyclodextrins for enhancing oral bioavailability. 2007;123:78–99. 

24.              Article R. an overview on solubility enhancement techniques for poorly soluble drugs and solid. 2012;3(04):942–56. 

25.              Arun K, Babu CJ, Laksmaiah P, Rao CB, Ravi B, Harshavardhan P. Techniques to Improve the Absorption of Poorly Soluble Drugs of Solubility. Int J Res Pharm Chem. 2012;2(2):533–40. 

26.              Chaudhary VB, Pharmacy SS. Chaudhary & Patel,. Cyclodext Incl Complex To Enhanc Solubility Poorly Water Soluble Drugs a Rev. 2013;4(1):68–76. 

27.              Sanghvi R, Evans D, Yalkowsky SH. Stacking complexation by nicotinamide: a useful way of enhancing drug solubility. Int J Pharm. 2007 May;336(1):35–41. 

28.              Higuchi T, Kristiansen H. Binding specificity between small organic solutes in aqueous solution: classification of some solutes into two groups according to binding tendencies. J Pharm Sci. 1970;59(11):1601–8. 

29.              Rajewski RA, Stella VJ. Pharmaceutical applications of cyclodextrins. 2. In vivo drug delivery. undefined. 1996;85(11):1142–69. 

30.              Ain S, Ain Q, Parveen S. an Overview on Various Approaches Used for Solubilization of Poorly Soluble Drugs. T Pharm Res. 2009;(2):84–104. 

31.              Marques HMC. A review on cyclodextrin encapsulation of essential oils and volatiles. Flavour Fragr J. 2010 Sep;25(5):313–26. 

32.              Astray G, Gonzalez-Barreiro C, Mejuto JC, Rial-Otero R, Simal-Gándara J. A review on the use of cyclodextrins in foods. Food Hydrocoll. 2009 Oct;23(7):1631–40. 

33.              Del Valle EMM. Cyclodextrins and their uses: a review. Process Biochem. 2004 May;39(9):1033–46. 

34.              Loftsson, T. and Brewster, M.E. (1996) Pharmaceutical Applications of Cycldextrins. 1. Drug Solubilization and Stabilization. Journal of Pharamceutical Science, 85, 10171025. - References - Scientific Research Publishing. 

35.              Gabelica V, Galic N, De Pauw E. On the specificity of cyclodextrin complexes detected by electrospray mass spectrometry. J Am Soc Mass Spectrom. 2002 Aug;13(8):946–53. 

36.              Loftsson T, Brewster ME, Másson M. Role of cyclodextrins in improving oral drug delivery. Am J Drug Deliv. 2004;2(4):261–75. 

37.              Loftsson T, Magnúsdóttir A, Másson M, Sigurjónsdóttir JF. Self-association and cyclodextrin solubilization of drugs. J Pharm Sci. 2002 Nov;91(11):2307–16. 

38.              Loftsson T, Duchˆ D. Cyclodextrins and their pharmaceutical applications. 2007;329:1–11. 

39.              Loftsson T, Brewster ME. Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization. J Pharm Sci. 1996 Oct;85(10):1017–25. 

40.              Suvarna V, Gujar P, Murahari M. ScienceDirect Complexation of phytochemicals with cyclodextrin derivatives – An insight. Biomed Pharmacother [Internet]. 2017;88:1122–

44. Available from: http://dx.doi.org/10.1016/j.biopha.2017.01.157

41.              Stella VJ, Rajewski RA. Cyclodextrins: their future in drug formulation and delivery. Pharm Res. 1997;14(5):556–67. 

42.              Kwon Y, Kim H, Park S, Jung S. Enhancement of Solubility and Antioxidant Activity of Some Flavonoids Based on the Inclusion Complexation with Sulfobutylether β Cyclodextrin. 2010;31(10):3035–7. 

43.              Carneiro SB, Duarte FÍC, Heimfarth L, Quintans JDSS, Quintans-Júnior LJ, Júnior VFDV, et al. Cyclodextrin–Drug Inclusion Complexes: In Vivo and In Vitro Approaches. Int J Mol Sci 2019, Vol 20, Page 642. 2019 Feb;20(3):642. 

44.              Pinho E, Grootveld M, Soares G, Henriques M. Cyclodextrins as encapsulation agents for plant bioactive compounds. Carbohydr Polym. 2014;101(1):121–35. 

45.              Duarte A, Martinho A, Luís Â, Figueiras A, Oleastro M, Domingues FC, et al. Resveratrol encapsulation with methyl-β-cyclodextrin for antibacterial and antioxidant delivery applications. LWT - Food Sci Technol. 2015 Oct;63(2):1254–60. 

46.              D’Aria F, Serri C, Niccoli M, Mayol L, Quagliariello V, Iaffaioli RV, et al. Host–guest inclusion complex of quercetin and hydroxypropyl-β-cyclodextrin. J Therm Anal Calorim 2017 1301. 2017 Feb;130(1):451–6. 

47.              Wei Y, Zhang J, Memon AH, Liang H. Molecular model and in vitro antioxidant activity of a water-soluble and stable phloretin/hydroxypropyl-β-cyclodextrin inclusion complex. J Mol Liq. 2017 Jun;236:68–75. 

48.              Dahabra L, Broadberry G, Gresley A Le, Najlah M. Sunscreens Containing Cyclodextrin Inclusion Complexes for Enhanced Efficiency : A Strategy for Skin Cancer Prevention. 2021;1–22. 

49.              Viernstein H, Weiss-greiler P, Wolschann P. Solubility enhancement of low soluble biologically active compounds — temperature and cosolvent dependent inclusion complexation. 2003;256:85–94. 

50.              Varandal AB, Magar DD, Saudagar RB. Different approaches toward the enhancement of Drug Solubility: A Review. J Adv Pharm Educ Res. 2013;3(4):415–26. 

51.              Carvalho YMBG, Menezes PP, Sousa BMH, Lima BS, Trindade IAS, Serafini MR, et al. Inclusion complex between β-cyclodextrin and hecogenin acetate produces superior analgesic effect in animal models for orofacial pain. Biomed Pharmacother. 2017;93:754–62. 

52.              Patil JS, Kadam D V., Marapur SC, Kamalapur M V. Inclusion complex system; a novel technique to improve the solubility and bioavailability of poorly soluble drugs: A review. Int J Pharm Sci Rev Res. 2010;2(2):29–34. 

53.              Ain S, Gupta V, K B, Ain Q, Dahiya J. Solubility Enhancement of the Poorly WaterSoluble Antiulcer Drug Famotidine by Inclusion Complexation. Int J Pharm Sci Nanotechnol. 2013 May;6(1):1983–9. 

54.              Banjare MK, Banjare RK, Behera K, Pandey S, Mundeja P, Ghosh KK. Inclusion complexation of novel synthesis amino acid based ionic liquids with β-cyclodextrin. J Mol Liq. 2020;299:112204. 

55.              Arima H, Yunomae K, Miyake K, Irie T, Hirayama F, Uekama K. Comparative studies of the enhancing effects of cyclodextrins on the solubility and oral bioavailability of tacrolimus in rats. J Pharm Sci. 2001;90(6):690–701. 

56.              Veiga F, Fernandes C, Teixeira F. Oral bioavailability and hypoglycaemic activity of tolbutamide/cyclodextrin inclusion complexes. Int J Pharm. 2000 Jul;202(1–2):165–71. 

57.              Miyake K, Arima H, Hirayama F, Yamamoto M, Horikawa T, Sumiyoshi H, et al. Improvement of solubility and oral bioavailability of rutin by complexation with 2hydroxypropyl-β-cyclodextrin. Pharm Dev Technol. 2000;5(3):399–407. 

58.              Loftsson T, Brewster ME. Cyclodextrins as Functional Excipients : Methods to Enhance Complexation Efficiency. 2012;101(9):10–2. 

59.              Cid-samamed A, Rakmai J, Carlos J, Simal-gandara J, Astray G. Cyclodextrins inclusion complex : Preparation methods , analytical techniques and food industry applications. Food Chem [Internet]. 2022;384(August 2021):132467. Available from: https://doi.org/10.1016/j.foodchem.2022.132467

60.              Fernandes CM, Veiga FJB. Effect of the hydrophobic nature of triacetyl-betacyclodextrin on the complexation with nicardipine hydrochloride: physicochemical and dissolution properties of the kneaded and spray-dried complexes. Chem Pharm Bull (Tokyo). 2002 Dec;50(12):1597–602. 

61.              Cunha-Filho MSS, Dacunha-Marinho B, Torres-Labandeira JJ, Martínez-Pancheco R, Landín M. Characterization of beta-lapachone and methylated beta-cyclodextrin solidstate systems. AAPS PharmSciTech. 2007 Jul;8(3). 

62.              Patel R, Bhimani D, Patel J, Patel D. Solid-state characterization and dissolution properties of ezetimibe-cyclodextrins inclusion complexes. J Incl Phenom Macrocycl Chem. 2008;60(3–4):241–51. 

63.              Kiran T, Shastri N, Ramakrishna S, Sadanandam M. surface solid dispersion of glimepiride for enhancement of dissolution rate. 2009; 

64.              Sheetal Z Godse MS, Patil, Swapnil M Kothavade RBS. Techniques for solubility enhancement of Hydrophobic drugs : A Review. J Adv Pharm Educ Res. 2013;3(4):403–14. 

65.              Cao F, Guo J, Ping Q. The physicochemical characteristics of freeze-dried scutellarincyclodextrin tetracomponent complexes. Drug Dev Ind Pharm. 2005;31(8):747–56. 

66.              Patel VR, Agrawal Y. Nanosuspension: An approach to enhance solubility of drugs. J Adv Pharm Technol Res. 2011;2(2):81. 

67.              Celebioglu A, Uyar T, Uyar T. Development of Ferulic Acid / Cyclodextrin Inclusion Complex Nanofibers for Fast-Dissolving Drug Delivery System. 2020; 

68.              Anjum MM, Patel KK, Pandey N, Tilak R, Agrawal AK, Singh S. Development of Anacardic Acid/hydroxypropyl-β-cyclodextrin inclusion complex with enhanced solubility and antimicrobial activity. J Mol Liq. 2019;296(xxxx). 

69.              Goyal G, Phukan AC, Hussain M, Lal V, Modi M, Goyal MK, et al. Water-soluble complexes of orange pigments from Monascus sp. with HP-β-CD: Preparation, inclusion mechanism, and improved stability, Jo ur na l P. J Neurol Sci. 2019;116544. 

70.              Uyar* AC and T. Development of Ferulic Acid/Cyclodextrin Inclusion Complex Nanofibers for Fast-Dissolving Drug Delivery System. Int J Pharm. 2020.

71.              Frangou M, Vlugt TJH, Moultos OA, Erd M. β -cyclodextrin : Ibuprofen in aqueous solutions ; A molecular dynamics simulation study. 2021;528. 

72.              Celebioglu A, Uyar T. Fast-dissolving antioxidant curcumin / cyclodextrin inclusion complex electrospun nano fi brous webs. 2020;317(February). 

73.              Loh GOK, Tan YTF, Peh KK. Enhancement of norfloxacin solubility via inclusion complexation with β-cyclodextrin and its derivative hydroxypropyl-β-cyclodextrin.

Asian J Pharm Sci. 2016;11(4):536–46. 

74.              Gao S, Jiang J, Li X, Ye F, Fu Y, Zhao L. An environmentally safe formulation with enhanced solubility and fungicidal activity : Self-assembly and characterization of Difenoconazole- β -CD inclusion complex. 2021;327. 

75.              Mohandoss S, Palanisamy S, You SG, Shim JJ, Rok Lee Y. Ultrasonication-assisted host–guest inclusion complexes of β-cyclodextrins and 5-hydroxytryptophan: Enhancement of water solubility, thermal stability, and in vitro anticancer activity. J Mol Liq. 2021;336. 

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