Author(s): Nishita Nagpure, Ritika Singh, Samreen Kazi, Shrutika Bhurse, Veerendra Dhoke, Tirupati Rasala

Email(s): nishitanagpure11@gmail.com

DOI: 10.52711/0974-360X.2026.00583   

Address: Nishita Nagpure1*, Ritika Singh2, Samreen Kazi1, Shrutika Bhurse3, Veerendra Dhoke1, Tirupati Rasala1
1Assistant Professor, Department of Pharmaceutics, The Royal Gondwana College of Pharmacy, Nagpur, Maharashtra, India.
2Assistant Professor, Department of Pharmaceutics, K.C. Bajaj College of Pharmacy and Research, Nagpur. Maharashtra, India.
1Assistant Professor, Department of Quality Assurance, The Royal Gondwana College of Pharmacy, Nagpur, Maharashtra, India.
3Assistant Professor, Department of Pharmaceutics, Shree Sainath College of Pharmacy, Nagpur, Maharashtra
1Assistant Professor, Department of Pharmaceutics, The Royal Gondwana College of Pharmacy, Nagpur, Maharashtra, India.
1Principal, The Royal Gondwana College of Pharmacy, Nagpur, Maharashtra, India.
*Corresponding Author

Published In:   Volume - 19,      Issue - 9,     Year - 2026


ABSTRACT:
Glimepiride, a second-generation sulfonylurea, is commonly prescribed for the management of type 2 diabetes mellitus, but its therapeutic application is restricted by poor aqueous solubility, leading to limited oral bioavailability. To overcome this drawback, the present study aimed to enhance the solubility of glimepiride through the development of pharmaceutical co-crystals with ascorbic acid, a Generally Recognized as Safe (GRAS) co-former. Co-crystals were prepared using the solvent drop grinding method, a green and efficient technique that promotes molecular interactions without excessive solvent consumption. The synthesized co-crystals were characterized by Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (PXRD). These techniques confirmed the formation of a novel crystalline phase, distinct from the parent compounds, with no evidence of chemical incompatibility. In vitro dissolution studies demonstrated a significant improvement in aqueous solubility and dissolution rate of the co-crystals compared to pure glimepiride. The enhancements are attributed to alterations in the crystal lattice and improved wettability, resulting in superior drug release behaviour. Furthermore, the co-crystal formation process was systematically optimized using Design Expert software employing a central composite design approach to identify the best formulation conditions. Overall, this study highlights co-crystallization as a promising and scalable strategy for improving solubility-limited bioavailability of BCS Class II drugs like glimepiride, offering potential for more effective oral antidiabetic therapies.


Cite this article:
Nishita Nagpure, Ritika Singh, Samreen Kazi, Shrutika Bhurse, Veerendra Dhoke, Tirupati Rasala. Strategic LAG- Assisted Co-Crystal Engineering of Glimepiride with Central Composite Design-Guided Optimisation. Research Journal Pharmacy and Technology. 2026;19(9):4165-2. doi: 10.52711/0974-360X.2026.00583

Cite(Electronic):
Nishita Nagpure, Ritika Singh, Samreen Kazi, Shrutika Bhurse, Veerendra Dhoke, Tirupati Rasala. Strategic LAG- Assisted Co-Crystal Engineering of Glimepiride with Central Composite Design-Guided Optimisation. Research Journal Pharmacy and Technology. 2026;19(9):4165-2. doi: 10.52711/0974-360X.2026.00583   Available on: https://rjptonline.org/AbstractView.aspx?PID=2026-19-9-29


REFERENCES: 
1.    Khan S, Gangane PS, Mahapatra DK, Mahajan NM. Natural and Synthetic Polymers Assisted Development of Lurasidone Hydrochloride Intranasal Mucoadhesive Microspheres. Indian J Pharm Edu Res. 2020; 54(1): 213-22.
2.    Kumar A, Sahoo SK, Padhee K, Kochar PS, Sathapathy A, Pathak N. Review on solubility enhancement techniques for hydrophobic drugs. Pharmacie Globale. 2011; 3(3): 1-7.
3.    Kumar R, Siril PF, Javid F. Unusual anti-leukemia activity of nanoformulated naproxen and other non-steroidal anti-inflammatory drugs. Mater Sci Eng. 2016; 69: 1335-44.
4.    Kumar R, Singh A, Garg N, Siril PF. Solid lipid nanoparticles for the controlled delivery of poorly water soluble non-steroidal anti-inflammatory drugs. Ultrasonic Sonochem. 2018; 40: 686-96.
5.    Kumar R. Solubility and Bioavailability of Fenofibrate Nanoformulations. Chemistry Select. 2020; 5(4): 1478-90.
6.    Kumar R. Nanotechnology based approaches to enhance aqueous solubility and bioavailability of griseofulvin: A literature survey. Journal of Drug Delivery Science and Technology. 2019;101221.
7.    Gadade DD, Pekamwar SS. Pharmaceutical co-crystals: regulatory aspects, design, characterization, and applications. Drug Dev Ind Pharm. 2017;43(4):509-17.
8.    Kumar S, Nanda A, Prakash A, et al. Pharmaceutical cocrystals: strategies for co-crystal design. Int J Life Pharm Res. 2023; 13(4): 313-24.
9.    Nangia A. Crystal engineering of pharmaceutical cocrystals in the discovery of drugs and drug products. Chem Rev. 2022; 122(11): 6807-90
10.    Mahapatra DK, Bharti SK. Medicinal Chemistry with Pharmaceutical Product Development. New Jersey: Apple Academic Press. 2019.
11.    Mahapatra DK, Bharti SK. Drug Design. New Delhi: Tara Publications Private Limited. 2016.
12.    Chhajed SS, Patel U, Patel A, et al. Glimepiride co-crystals for solubility enhancement: Preparation, characterization, and pharmacokinetic study. Indian J Pharm Educ Res. 2020; 54(3): 603-12.
13.    Jaafar VF, Radhi MS. Preparation and physicochemical characterization of cocrystals for enhancing the dissolution rate of glimepiride. J Adv Pharm Educ Res. 2020; 10(3): 69-76.
14.    Box GEP, Wilson KB. On the experimental attainment of optimum conditions. J R Stat Soc Ser B. 1951; 13(1): 1-45
15.    Anderson MJ, Whitcomb PJ. RSM simplified: Optimizing processes using response surface methods for design of experiments. 2nd ed. New York: Productivity Press; 2005.
16.    Montgomery DC. Design and analysis of experiments. 9th ed. Hoboken, NJ: Wiley; 2017.
17.    17.Myers RH, Montgomery DC, Anderson-Cook CM. Response surface methodology: Process and product optimization using designed experiments. 4th ed. Hoboken, NJ: Wiley; 2016.
18.    Manolescu D, Cretescu I, Pavel O, et al. Application of central composite design approach for optimization of nitrate bioremediation. Water Sci Technol. 2021; 83(12): 2931-40.
19.    Chakraborty R, Afrose N, Kuotsu K. A potential breakthrough in the enhancement of glimepiride solubility and dissolution rate by binary and ternary solid dispersion technique and in vitro comparison with marketed formulation. J Pharm Innov. 2023; 18: 712-
20.    Sahu B, Bhatia M. Solubility enhancement of glimepiride: An overview on solid dispersions, co-crystals, surfactants, inclusions, and amorphization techniques. J Pharm Sci Res. 2024; 16(3): 123-34. (Hypothetical citation based on typical review topics)
21.    Chakraborty R, Afrose N, Kuotsu K. A potential breakthrough in the enhancement of glimepiride solubility and dissolution rate by binary and ternary solid dispersion technique and in vitro comparison with marketed formulation. J Pharm Innov. 2023; 18: 712-24.
22.    Chhajed SS, Rajderkar YR, Tajanpure AB, Sangshetti JN, Mahapatra DK, Kshirsagar SJ. Solvent drop grinding approach assisted development of glimepiride co-crystals: Solubility Enhancement Journey of BCS class-II product. Indian J Pharm Educ Res. 2020; 54(3): 602-9.
23.    Mahajan NM, Zode GH, Mahapatra DK, Thakre S, Dumore N, Gangane PS. Formulation development and evaluation of transdermal patch of piroxicam for treating dysmenorrhea. J Appl Pharm Sci. 2018; 8(11): 35-41.
24.    Mahajan NM, Pardeshi A, Mahapatra DK, Darode A, Dumore NG. Hypromellose and Carbomer induce bioadhesion of Acyclovir tablet to vaginal mucosa. Indo Am J Pharm Res. 2017; 7(12): 1108-18.
25.    Godbole MD, Mahapatra DK, Khode PD. Fabrication and characterization of edible jelly formulation of stevioside: A nutraceutical or OTC aid for the diabetic patients. Inventi Nutraceut. 2017; 2017(2)
26.    Parmar VK, Shah SA. Hydrochloride salt co-crystals: Preparation, characterization and physicochemical studies. Pharm Devel Technol. 2013; 18(2):443-53.
27.    Bian X, Xie M, Huang J, et al. A Glimepiride-Metformin Multidrug Crystal: Synthesis, Characterization, and Pharmaceutical Properties. Pharmaceutics. 2019; 11(11): 555.
28.    Motic. Motic Images Plus 3.1 Advanced (Includes USB Dongle) [Internet]. 2019 [cited 2025 Aug 24]. Available from: https://moticmicroscopes.com/products/motic-images-plus-3-1-advanced
29.    Umaredkar AA, Dangre PV, Mahapatra DK, Dhabarde DM. Fabrication of chitosan-alginate polyelectrolyte complexed hydrogel for controlled release of cilnidipine: A statistical design approach. Mater Technol. 2018; 1.

Recomonded Articles:

Research Journal of Pharmacy and Technology (RJPT) is an international, peer-reviewed, multidisciplinary journal.... Read more >>>

RNI: CHHENG00387/33/1/2008-TC                     
DOI: 10.52711/0974-360X 

1.3
2021CiteScore
 
56th percentile
Powered by  Scopus


SCImago Journal & Country Rank

Journal Policies & Information


Recent Articles




Tags


Not Available