Author(s):
Chetan Hasmukh Mehta, Poojary Pooja Srinivas, Anusha SB, Kirollos Bahaa Fathy Mahany, KB Koteshwara, Usha Yogendra Nayak
Email(s):
usha.nayak@manipal.edu
DOI:
10.52711/0974-360X.2022.00622 
Address:
Chetan Hasmukh Mehta1, Poojary Pooja Srinivas1, Anusha SB1, Kirollos Bahaa Fathy Mahany2, KB Koteshwara1, Usha Yogendra Nayak1*
1Department of Pharmaceutics, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka 576104, India.
2Faculty of Pharmacy, Assiut University, Egypt.
*Corresponding Author
Published In:
Volume - 15,
Issue - 8,
Year - 2022
ABSTRACT:
The present study is aimed at the design and development of aceclofenac co-crystals. Co-crystallization is one of the important techniques which helps to enhance the aqueous solubility of drugs by modifying the crystal structure using incorporation of the co-former into the formulation.. In the present study, supramolecular synthon approach and computational grid scan methods were used for the co-former selection. The different co-formers such as oxalic acid (OA), succinic acid (SA), maleic acid (MA), and benzoic acid (BA) were used. Aceclofenac (ACF) co-crystals were prepared by solvent evaporation and dry grinding method. Based on the computational results and experimental saturation solubility studies, maleic acid was considered as the suitable co-former for the preparation. The solid-state characterization showed partial conversion of ACF crystallinity to the amorphization as evident from the decrease in peak intensity and the number of peaks. The co-crystals showed increased aqueous solubility of ACF and higher drug release in basic pH. All the characterization parameters proved the co-crystal formation and the in vitro release studies showed that the solubility enhancement of the ACF by preparing ACF-MA co-crystals. Thus, it can be concluded that co-crystallization is one of the novel method for improving the bioavailability of aceclofenac.
Cite this article:
Chetan Hasmukh Mehta, Poojary Pooja Srinivas, Anusha SB, Kirollos Bahaa Fathy Mahany, KB Koteshwara, Usha Yogendra Nayak. Computational and Experimental Insights in Design and Development of Aceclofenac Co-Crystals. Research Journal of Pharmacy and Technology. 2022; 15(8):3709-6. doi: 10.52711/0974-360X.2022.00622
Cite(Electronic):
Chetan Hasmukh Mehta, Poojary Pooja Srinivas, Anusha SB, Kirollos Bahaa Fathy Mahany, KB Koteshwara, Usha Yogendra Nayak. Computational and Experimental Insights in Design and Development of Aceclofenac Co-Crystals. Research Journal of Pharmacy and Technology. 2022; 15(8):3709-6. doi: 10.52711/0974-360X.2022.00622 Available on: https://rjptonline.org/AbstractView.aspx?PID=2022-15-8-64
REFERENCES:
1. Thorat YS, Gonjari ID, Hosmani AH. Solubility Enhancement Techniques: A Review On Conventional And Novel Approaches. Int. J. Pharm. Sci. Res. 2011; 2(10):2501-2513. Www.Ijpsr.Com. Accessed December 16, 2019.
2. Christopher Vimalson D, Parimalakrishnan S, Jeganathan NS, Anbazhagan S. Techniques To Enhance Solubility Of Hydrophobic Drugs: An Overview. Asian J Pharm. 2016; 10(2):S67-S75. Doi:10.22377/Ajp.V10i2.625
3. Amidon GL, Lennernäs H, Shah VP, Crison JR. A Theoretical Basis For A Biopharmaceutic Drug Classification: The Correlation Of In Vitro Drug Product Dissolution And In Vivo Bioavailability. Pharm Res. 1995; 12(3):413-420. Doi:10.1023/A:1016212804288
4. Kumar S, Nanda A. Pharmaceutical Cocrystals: An Overview. Indian J Pharm Sci. 2017; 79(6):858-871. Doi:10.4172/Pharmaceutical-Sciences.1000302
5. Yadav A V., Shete AS, Dabke AP, Kulkarni P V., Sakhare SS. Co-Crystals: A Novel Approach To Modify Physicochemical Properties Of Active Pharmaceutical Ingredients. Indian J Pharm Sci. 2009; 71(4):359-370. Doi:10.4103/0250-474X.57283
6. Krishnaiah YS. Pharmaceutical Technologies For Enhanc-Ing Oral Bioavailability Of Poorly Soluble Drugs. J Bioequiv Availab. 2010; 2(2):28-036. Doi:10.4172/Jbb.1000027
7. Savjani KT, Gajjar AK, Savjani JK. Drug Solubility: Importance And Enhancement Techniques. ISRN Pharm. 2012; 2012:1-10. Doi:10.5402/2012/195727
8. Kotak U, Prajapati V, Solanki H, Jani G, Jha P. Co-Crystallization Technique Its Rationale And Recent Progress. World J Pharm Pharm Sci. 2015:4(4); 1484-1508. Www.Wjpps.Com. Accessed December 15, 2019.
9. Patole Tanvee, Deshpande Ashwini. Co-Crystallization- A Technique For Solubility Enhancement. Int J Pharm Sci Res. 2014; 5(9):3566-3576. Doi:10.13040/IJPSR.0975-8232.5(9).3566-76
10. Fda, Cder, Stewart, Felicia. Regulatory Classification Of Pharmaceutical Co-Crystals Guidance For Industry. Http://Www.Fda.Gov/Drugs/Guidancecomplianceregulatoryinformation/Guidances/Default.Htm. Published 2018. Accessed May 5, 2018.
11. Nijhawan M, Sathesh Babu PR, Subrahmanyam CVS. Cocrystals Of Irbesartan With Hippuric Acid. Indo Am J Pharm Res. 2015; 5(4):1323-1329. Https://Www.Ejmanager.Com/Mnstemps/36/36-1430993585.Pdf. Accessed May 5, 2018.
12. Othman MF, Anuar N, Ad Rahman S, Ahmad Taifuddin NA. Cocrystal Screening Of Ibuprofen With Oxalic Acid And Citric Acid Via Grinding Method. In: IOP Conference Series: Materials Science And Engineering. Vol 358. Institute Of Physics Publishing; 2018. Doi:10.1088/1757-899X/358/1/012065
13. Issa N, Barnett SA, Mohamed S, Et Al. Screening For Cocrystals Of Succinic Acid And 4-Aminobenzoic Acid. Crystengcomm. 2012; 14(7):2454-2464. Doi:10.1039/C2ce06325e
14. Taylor CR, Day GM. Evaluating The Energetic Driving Force For Cocrystal Formation. Cryst Growth Des. 2018; 18(2):892-904. Doi:10.1021/Acs.Cgd.7b01375
15. Mohamed S, Tocher DA, Price SL. Computational Prediction Of Salt And Cocrystal Structures - Does A Proton Position Matter? Int J Pharm. 2011; 418(2):187-198. Doi:10.1016/J.Ijpharm.2011.03.063
16. Issa N, Karamertzanis PG, Welch GWA, Price SL. Can The Formation Of Pharmaceutical Cocrystals Be Computationally Predicted? I. Comparison Of Lattice Energies. Cryst Growth Des. 2009; 9(1):442-453. Doi:10.1021/Cg800685z
17. Karamertzanis PG, Kazantsev A V., Issa N, Et Al. Can The Formation Of Pharmaceutical Cocrystals Be Computationally Predicted? 2. Crystal Structure Prediction. J Chem Theory Comput. 2009; 5(5):1432-1448. Doi:10.1021/Ct8004326
18. Varma A, Laxmi P, Pai A, Pai G, SG V, Badamane Sathyanarayana M. Designing Of Stable Co-Crystals Of Zoledronic Acid Using Suitable Coformers. Chem Pharm Bull. 2019; 67(8):816-823. Doi:10.1248/Cpb.C19-00202
19. Verma S, Nanda A, Basu SP. Screening, Preparation, And Characterization Of Aceclofenac Cocrystals. Drug Invent Today. 2019; 11:81-87.
20. Mutalik S, Anju P, Manoj K, Usha AN. Enhancement Of Dissolution Rate And Bioavailability Of Aceclofenac: A Chitosan-Based Solvent Change Approach. Int J Pharm. 2008; 350(1-2):279-290. Doi:10.1016/J.Ijpharm.2007.09.006
21. Usha AN, Mutalik S, Reddy MS, Ranjith AK, Kushtagi P, Udupa N. Preparation And, In Vitro, Preclinical And Clinical Studies Of Aceclofenac Spherical Agglomerates. Eur J Pharm Biopharm. 2008; 70(2):674-683. Doi:10.1016/J.Ejpb.2008.06.010
22. Narayan R, Pednekar A, Bhuyan D, Gowda C, Koteshwara KB, Nayak UY. A Top-Down Technique To Improve The Solubility And Bioavailability Of Aceclofenac: In Vitro And In Vivo Studies. Int J Nanomedicine. 2017; 12:4921-4935. Doi:10.2147/IJN.S141504
23. Maulvi FA, Dalwadi SJ, Thakkar VT, Soni TG, Gohel MC, Gandhi TR. Improvement Of Dissolution Rate Of Aceclofenac By Solid Dispersion Technique. Powder Technol. 2011; 207(1-3):47-54. Doi:10.1016/J.Powtec.2010.10.009
24. Ranpise NS, Kulkarni NS, Mair PD, Ranade AN. Improvement Of Water Solubility And In Vitro Dissolution Rate Of Aceclofenac By Complexation With Β-Cyclodextrin And Hydroxypropyl-Β-Cyclodextrin. Pharm Dev Technol. 2010; 15(1):64-70. Doi:10.3109/10837450903002165
25. Dua K, Pabreja K, Ramana M V. Enhancement Of Dissolution Behavior Of Aceclofenac By Complexation With Β-Cyclodextrin-Choline Dichloride Coprecipitate. J Dispers Sci Technol. 2011; 32(10):1477-1484. Doi:10.1080/01932691.2010.513317
26. Pattnaik S, Swain K, Manaswini P, Et Al. Fabrication Of Aceclofenac Nanocrystals For Improved Dissolution: Process Optimization And Physicochemical Characterization. J Drug Deliv Sci Technol. 2015; 29:199-209. Doi:10.1016/J.Jddst.2015.07.021
27. Park JJ, Meghani N, Choi JS, Lee BJ. Development And Evaluation Of Decorated Aceclofenac Nanocrystals. Colloids Surfaces B Biointerfaces. 2016; 143:206-212. Doi:10.1016/J.Colsurfb.2016.03.022
28. Rahim Haroon, Sadiq Abdul, Khan Shahzeb, Et Al. Aceclofenac Nanocrystals With Enhanced In Vitro In Vivo Performance: Formulation Optimization, Characterization, Analgesic And Acute Toxicity Studies. Drug Des Devel Ther. 2017; 11:2443-2452. Doi:10.2147/DDDT.S140626
29. Sodanapalli Riyaz, Nair Rahul, Bachala Thanuja. Synthesis And Characterization Of A Pharmaceutical Co-Crystal: (Aceclofenac: Nicotinamide). Int. J. Pharm. Sci. Res. 2011:3(6); 1288.
30. Goud NR, Suresh K, Nangia A. Solubility And Stability Advantage Of Aceclofenac Salts. Cryst Growth Des. 2013; 13(4):1590-1601. Doi:10.1021/Cg301825u
31. Chandel N, Gupta V, Pandey A, Saxena S, Choudhary S. Co-Crystalization Of Aceclofenac And Paracetamol And Their Characterization. Int J Pharm Life Sci. 2011; 2(8):1020-1028.
32. Sohrab M, Mahapatra SP, Tiwari S. Enhancement Of Dissolution Rate Of Aceclofenac By Formation Of Aceclofenac-Nicotinic Acid Cocrystal Using Water Soluble Polymers Like PVPK-30, HPMCE5, SSG And Na-CMC. Indo Glob J Pharm Sci. 2015; 5(3):154-170.
33. Panzade P, Shendarkar G, Shaikh S, Rathi PB. Pharmaceutical Cocrystal Of Piroxicam: Design, Formulation And Evaluation. Adv Pharm Bull. 2017; 7(3):399-408. Doi:10.15171/Apb.2017.048
34. Karimi-Jafari M, Padrela L, Walker GM, Croker DM. Creating Cocrystals: A Review Of Pharmaceutical Cocrystal Preparation Routes And Applications. Cryst. Growth Des. 2018:18(10); 6370-6387. Doi:10.1021/Acs.Cgd.8b00933
35. Chadwick K, Davey R, Cross W. How Does Grinding Produce Co-Crystals? Insights From The Case Of Benzophenone And Diphenylamine. Crystengcomm. 2007; 9(9):732-734. Doi:10.1039/B709411f
36. Ganesh M, Jeon UJ, Ubaidulla U, Et Al. Chitosan Cocrystals Embedded Alginate Beads For Enhancing The Solubility And Bioavailability Of Aceclofenac. Int J Biol Macromol. 2015; 74:310-317. Doi:10.1016/J.Ijbiomac.2014.12.038
37. Setyawan D, Sari R, Yusuf H, Primaharinastiti R. Preparation And Characterization Of Artesunate - Nicotinamide Cocrystal By Solvent Evaporation And Slurry Method. Asian J Pharm Clin Res. 2014:7(1); 62-65.
38. Shah K, Borhade S, Londhe V. Utilization Of Co-Crystallization For Solubility Enhancement Of A Poorly Soluble Antiretroviral Drug-Ritonavir. Int J Pharm Pharm Sci.; 2014:6(2)556-558. www.hiv-druginteractions.org,. Accessed December 19, 2019.