Enhancement of solubility and bioavailability of poorly water soluble drug
Abstract
More specifically, this work aims to investigate the cyclodextrin's complexation, solubility, dissolution rate, and efficacy in pharmaceutical formulations. The pharmacokinetic properties of cyclodextrin forms were also investigated. It's possible to increase the solubility of drug using cyclodextrine, demon strategic use of the term "solubility constant" to describe the effect on Lercin-3xtrin shows that the drug increases its phase solubility. It had a β-extrin concentration of 164.557 units per milliliter (eβ-extrin). The FT-IR studies demonstrated that all the ingredients used in making Lercanipariq included tablets were acceptable to immediate release. The dissolution of Lercidin became evident by Kneading inclusion test from complex LK2 was found to be greater than the pure substance or those made by other methods. The Lercandipine prepared with the inclusion complex system Kneading method, as well as tablets formulation F6 (F6 using Lercinium inclusion complex and Lanpirin 2% ingredients), failed to show any effect on physical appearance, drug content, and dissolution in short-character stability and profile tests. Thus, by solubilizing and thus enhancing, the lipid solubility, β-cyclodextrin has been shown to facilitate the release of Lercanipine.
Keywords:
β-extrin, FT-IR, Lercandipine, β-cyclodextrin
References
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19. Uppugalla S, Srinivasan P. High-performance supercapacitor coin cell: polyaniline and nitrogen, sulfur-doped activated carbon electrodes in aqueous electrolyte. Journal of Solid State Electrochemistry. 2019 Jan;23(1):295-306.
20. Uppugalla S, Srinivasan P. Polyaniline nanofibers and porous Ni [OH] 2 sheets coated carbon fabric for high performance super capacitor. Journal of Applied Polymer Science. 2019 Nov 5;136(41):48042.
21. Uppugalla S, Boddula R, Srinivasan P. Methyl triphenylphosphonium permanganate as a novel oxidant for aniline to polyaniline-manganese (II, IV) oxide: material for high performance pseudocapacitor. Journal of Solid State Electrochemistry. 2018 Feb;22(2):407-15.
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23. Boini, K.M., singh, A. and Koka, S.S., 2021. Gut Microbial Metabolite Trimethylamine N-oxide Enhances Endoplasmic Reticular Stress and Promotes Endothelial Dysfunction. Circulation, 144(Suppl_1), pp.A14071-A14071.
24. Hovgaard L, Bronsted H. Drug delivery studies in caco-2 monolayers. Absorption enhancer effects of cyclodextrins. Pharm Res. 1995; 12(9): 1328-1332.
25. Roh, J.D., Kitchen, R.R., Guseh, J.S., McNeill, J.N., Aid, M., Martinot, A.J., Yu, A., Platt, C., Rhee, J., Weber, B. and Trager, L.E., 2022. Plasma proteomics of COVID-19–associated cardiovascular complications: implications for pathophysiology and therapeutics. Basic to Translational Science, 7(5), pp.425-441MS. ZALAK R. PATEL, MRS. HETAL K. PATEL, MR. HARSH J. TRIVEDI, DR. KUNAL N. PATEL, and DR. BHAVESH S. NAYAK. “Enhancement of Solubility and Dissolution Properties of Lacidipine by Solid Dispersion”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 5, May 2015, pp. 165-70, https://www.ijpda.com/index.php/journal/article/view/154.
26. Surya Prakash Gautam, Arun Kumar Gupta, Shahid Ud Din Wani, Neelesh Malviya, Tapsya Gautam, and Anil Kumar Sharma. “PAMAM Dendrimers Mediated Solubility Enhancement of Poorly Soluble Drugs: A Concise Review”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 4, Apr. 2015, pp. 105-10, https://www.ijpda.com/index.php/journal/article/view/152.
27. Ankit Gupta, Mahesh Kumar Kataria, and Ajay Bilandi. “FORMULATION AND EVALUATION OF SOLID DISPERSION OF GLIPIZIDE FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT”. International Journal of Pharmaceutics and Drug Analysis, vol. 2, no. 2, Feb. 2014, pp. 74-87, https://www.ijpda.com/index.php/journal/article/view/21.
28. MS. ZALAK R. PATEL, MRS. HETAL K. PATEL, MR. HARSH J. TRIVEDI, DR. KUNAL N. PATEL, and DR. BHAVESH S. NAYAK. “Enhancement of Solubility and Dissolution Properties of Lacidipine by Solid Dispersion”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 5, May 2015, pp. 165-70, https://www.ijpda.com/index.php/journal/article/view/154.
29. Surya Prakash Gautam, Arun Kumar Gupta, Shahid Ud Din Wani, Neelesh Malviya, Tapsya Gautam, and Anil Kumar Sharma. “PAMAM Dendrimers Mediated Solubility Enhancement of Poorly Soluble Drugs: A Concise Review”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 4, Apr. 2015, pp. 105-10, https://www.ijpda.com/index.php/journal/article/view/152.
2. Singh, A., Srinivasan, A.K., Chakrapani, L.N. and Kalaiselvi, P., 2019. LOX-1, the common therapeutic target in hypercholesterolemia: a new perspective of antiatherosclerotic action of aegeline. Oxidative medicine and cellular longevity, 2019.
3. Aguiar MM, Rodrigues JM, Silva Cunha A. Encapsulation of insulin-cyclodextrin complex in PLGA microspheres: a new approach for prolonged pulmonary insulin delivery. J Microencapsul. 2004; 21(5): 553-64.
4. Singh, A., Gowtham, S., Chakrapani, L.N., Ashokkumar, S., Kumar, S.K., Prema, V., Bhavani, R.D., Mohan, T. and Sathyamoorthy, Y.K., 2018. Aegeline vs Statin in the treatment of Hypercholesterolemia: A comprehensive study in rat model of liver steatosis. Functional Foods in Health and Disease, 8(1), pp.1-16.
5. Loftsson Thorsteinn, Marcus E Brewster. Pharmaceutical applications of cyclodextrins. Journal of Pharmaceutical Sciences, 85(10), 1996, 1017-1026.
6. K.P.R. Chowdary and A.M.S. Sudhakar Babu. “A Factorial Study to Evaluate the Individual and Combined Effects of β-Cyclodextrin and Tween 80 on the Solubility and Dissolution Rate of Aceclofenac”. Asian Journal of Chemistry Vol.22, No. 6 (2010), 4281-4285.
7. Singh, A., Kumar, A. and Kalaiselvi, P., 2018. Aegeline, targets LOX1, the receptor for oxidized LDL to mitigate hypercholesterolemia: a new perspective in its anti-atherosclerotic action. Free Radical Biology and Medicine, 128, p.S41.
8. Singh, A., 2022. Role of microbial metabolites in cardiovascular and human health. In Microbiome, Immunity, Digestive Health and Nutrition (pp. 137-148). Academic Press.
9. Loftsson T, Magnusdottir A, Masson M, Sigurjonsdottir JF. Self-association and cyclodextrin solubilization of drugs, J Pharm Sci. 2002; 91(11):2307-2316.
10. Abhilasha, S., Narasimhan, C.L., Kumar, S.A., Kumar, S.N.K., Bhavani, R.D., Thangarajeswari, M., Prema, V. and Kalaiselvi, P., 2017. Ethanolic extract of aegle marmelos mediates its hypocholesterolemic effect by retarding circulatory oxidized ldl formation via 12/15 lipoxygenase pathway.
11. Attama AA et al. Studies on diclofenac β-cyclodextrin inclusion complexes. Journal of Pharmaceutical Research, July 2004; 3(3): 47-49.
12. Singh, A., 2022. Role of microbial metabolites in cardiovascular and human health. In Microbiome, Immunity, Digestive Health and Nutrition (pp. 137-148). Academic Press.
13. Sunil Jambhekar, Casella R, Maher T. The physicochemical characteristics and bioavailability of indomethacin from β-cyclodextrin, HE β-CD and HPβ-CDs complexes. Inter.J.270, 2004,149-166.
14. Shiv Chandra Singh, A., Yu, A., Chang, B., Li, H., Rosenzweig, A. and Roh, J.D., 2021. Exercise Training Attenuates Activin Type II Receptor Signaling in the Aged Heart. Circulation, 144(Suppl_1), pp.A14259-A14259.
15. Chowdary KPR, Vijaya Srinivas. Effect of polyvinyl pyrrolidone on complexation and dissolution rate of β and HPβ-CD complexes of celecoxib. Ind.J.Pharm.Sci. Sept-oct. 2006, 631-634.
16. Roh, J., Hill, J.A., Singh, A., Valero-Muñoz, M. and Sam, F., 2022. Heart failure with preserved ejection fraction: heterogeneous syndrome, diverse preclinical models. Circulation Research, 130(12), pp.1906-1925.
17. Uppugalla S, Male U, Srinivasan P. Design and synthesis of heteroatoms doped carbon/polyaniline hybrid material for high performance electrode in supercapacitor application. Electrochimica Acta. 2014 Nov 10;146:242-8.
18. Male U, Uppugalla S, Srinivasan P. Effect of reduced graphene oxide–silica composite in polyaniline: electrode material for high-performance supercapacitor. Journal of Solid State Electrochemistry. 2015 Nov;19(11):3381-8.
19. Uppugalla S, Srinivasan P. High-performance supercapacitor coin cell: polyaniline and nitrogen, sulfur-doped activated carbon electrodes in aqueous electrolyte. Journal of Solid State Electrochemistry. 2019 Jan;23(1):295-306.
20. Uppugalla S, Srinivasan P. Polyaniline nanofibers and porous Ni [OH] 2 sheets coated carbon fabric for high performance super capacitor. Journal of Applied Polymer Science. 2019 Nov 5;136(41):48042.
21. Uppugalla S, Boddula R, Srinivasan P. Methyl triphenylphosphonium permanganate as a novel oxidant for aniline to polyaniline-manganese (II, IV) oxide: material for high performance pseudocapacitor. Journal of Solid State Electrochemistry. 2018 Feb;22(2):407-15.
22. Sanjula Baboota, Dhaliwal M, Kohli K., et.al. Inclusion complexation of rofecoxib with dimethyl β-cyclodextrin. Ind. J. of Pharm. Sci. March-April 2005, 226-229.
23. Boini, K.M., singh, A. and Koka, S.S., 2021. Gut Microbial Metabolite Trimethylamine N-oxide Enhances Endoplasmic Reticular Stress and Promotes Endothelial Dysfunction. Circulation, 144(Suppl_1), pp.A14071-A14071.
24. Hovgaard L, Bronsted H. Drug delivery studies in caco-2 monolayers. Absorption enhancer effects of cyclodextrins. Pharm Res. 1995; 12(9): 1328-1332.
25. Roh, J.D., Kitchen, R.R., Guseh, J.S., McNeill, J.N., Aid, M., Martinot, A.J., Yu, A., Platt, C., Rhee, J., Weber, B. and Trager, L.E., 2022. Plasma proteomics of COVID-19–associated cardiovascular complications: implications for pathophysiology and therapeutics. Basic to Translational Science, 7(5), pp.425-441MS. ZALAK R. PATEL, MRS. HETAL K. PATEL, MR. HARSH J. TRIVEDI, DR. KUNAL N. PATEL, and DR. BHAVESH S. NAYAK. “Enhancement of Solubility and Dissolution Properties of Lacidipine by Solid Dispersion”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 5, May 2015, pp. 165-70, https://www.ijpda.com/index.php/journal/article/view/154.
26. Surya Prakash Gautam, Arun Kumar Gupta, Shahid Ud Din Wani, Neelesh Malviya, Tapsya Gautam, and Anil Kumar Sharma. “PAMAM Dendrimers Mediated Solubility Enhancement of Poorly Soluble Drugs: A Concise Review”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 4, Apr. 2015, pp. 105-10, https://www.ijpda.com/index.php/journal/article/view/152.
27. Ankit Gupta, Mahesh Kumar Kataria, and Ajay Bilandi. “FORMULATION AND EVALUATION OF SOLID DISPERSION OF GLIPIZIDE FOR SOLUBILITY AND DISSOLUTION RATE ENHANCEMENT”. International Journal of Pharmaceutics and Drug Analysis, vol. 2, no. 2, Feb. 2014, pp. 74-87, https://www.ijpda.com/index.php/journal/article/view/21.
28. MS. ZALAK R. PATEL, MRS. HETAL K. PATEL, MR. HARSH J. TRIVEDI, DR. KUNAL N. PATEL, and DR. BHAVESH S. NAYAK. “Enhancement of Solubility and Dissolution Properties of Lacidipine by Solid Dispersion”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 5, May 2015, pp. 165-70, https://www.ijpda.com/index.php/journal/article/view/154.
29. Surya Prakash Gautam, Arun Kumar Gupta, Shahid Ud Din Wani, Neelesh Malviya, Tapsya Gautam, and Anil Kumar Sharma. “PAMAM Dendrimers Mediated Solubility Enhancement of Poorly Soluble Drugs: A Concise Review”. International Journal of Pharmaceutics and Drug Analysis, vol. 3, no. 4, Apr. 2015, pp. 105-10, https://www.ijpda.com/index.php/journal/article/view/152.
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V, B., & N, A. (2021). Enhancement of solubility and bioavailability of poorly water soluble drug . Journal of Integral Sciences, 4(3), 1-19. Retrieved from https://jisciences.com/index.php/journal/article/view/34
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