Comparative Study of Hydrophilic Polymer-Based Solid Dispersions of Griseofulvin Incorporating HPMC E6, PVP K30, and Soluplus

Authors

  • Sarah Salim Oleiwi Department of Biopharmaceutics, College of Pharmacy, Mustansiriyah University, Iraq
  • Omar Sarheed School of pharmacy and Biomedical sciences, University of Central Lancashire, Preston, United Kingdom
  • Ghaidaa S. Hameed Department of Biopharmaceutics, College of Pharmacy, Mustansiriyah University, Iraq

DOI:

https://doi.org/10.32947/ajps.v26i2.1380

Keywords:

Amorphous, crystalline, Griseofulvin, Hydrophilic polymers, Solid dispersion

Abstract

Solid dispersion approach with hydrophilic carriers is one of the most effective methods for improving the solubility, dissolution profile, and ultimately the oral bioavailability of poorly water-soluble drugs. In this study, Griseofulvin (GF), a BCS class II drug with poor solubility and a strong tendency to recrystallize, was formulated using hydrophilic polymers (HPMC E6, Polyvinylpyrrolidone K30 (PVP), and Soluplus) at drug to polymer ratios of 1:2, 1:3, and 1:4 using the solvent evaporation method.

An experimental polymer-selection approach was employed to determine the optimal carrier type and ratio, wherein drug–polymer compatibility studies (FTIR), solid-state characterization (PXRD), saturated solubility studies, and dissolution behavior were systematically evaluated. The 1:3 HPMC formula demonstrated the most favorable performance, showing superior saturated solubility, enhanced dissolution rate, and good stability at harsh conditions across 90 days. This formulation represents a promising approach for improving the biopharmaceutical properties of Griseofulvin.

References

1- DeBoyace K. Modeling and Prediction of Amorphous Solid Dispersion Formation Using a Molecular Descriptor: Duquesne University; 2019.

2- Pandi P, Bulusu R, Kommineni N, Khan W, Singh M. Amorphous solid dispersions: An update for preparation, characterization, mechanism on bioavailability, stability, regulatory considerations and marketed products. Int J Pharm. 2020;586:119560.

3- Trasi NS, Bhujbal S, Zhou QT, Taylor LS. Amorphous solid dispersion formation via solvent granulation–A case study with ritonavir and lopinavir. International journal of pharmaceutics: X. 2019;1:100035.

4- França MT, Marcos TM, Pereira RN, Stulzer HK. Could the small molecules such as amino acids improve aqueous solubility and stabilize amorphous systems containing Griseofulvin? European Journal of Pharmaceutical Sciences. 2020;143:105178.

5- Pas T, Struyf A, Vergauwen B, Van den Mooter G. Ability of gelatin and BSA to stabilize the supersaturated state of poorly soluble drugs. European Journal of Pharmaceutics and Biopharmaceutics. 2018;131:211-23.

6- Zheng K, Lin Z, Capece M, Kunnath K, Chen L, Davé RN. Effect of particle size and polymer loading on dissolution behavior of amorphous griseofulvin powder. Journal of pharmaceutical sciences. 2019;108(1):234-42.

7- Sarode AL, Sandhu H, Shah N, Malick W, Zia H. Hot melt extrusion (HME) for amorphous solid dispersions: Predictive tools for processing and impact of drug–polymer interactions on supersaturation. European Journal of Pharmaceutical Sciences. 2013;48(3):371-84.

8- Chen Y, Liu C, Chen Z, Su C, Hageman M, Hussain M, et al. Drug–polymer–water interaction and its implication for the dissolution performance of amorphous solid dispersions. Molecular pharmaceutics. 2015;12(2):576-89.

9- Malkawi R, Malkawi WI, Al-Mahmoud Y, Tawalbeh J. Current trends on solid dispersions: past, present, and future. Advances in Pharmacological and Pharmaceutical Sciences. 2022;2022(1):5916013.

10- Shi Q, Chen H, Wang Y, Wang R, Xu J, Zhang C. Amorphous solid dispersions: role of the polymer and its importance in physical stability and in vitro performance. Pharmaceutics. 2022;14(8):1747.

11- Naama NA, Hameed GS, Hanna DB, Mahdi ZH. Formulation of Cefdinir Ternary Solid Dispersion and Stability Study under Harsh Conditions. Al Mustansiriyah Journal of Pharmaceutical Sciences. 2025;25(1):27-48.

12- Hussein AM, Hameed G, Aziz FM. Improve the solubility of cefpodoxime proxetil by amorphous solid dispersion technique. Journal of Research in Pharmacy. 2025;29(4):1437-50.

13- Hatem AQ, Ali WK. Preparation and Characterization of Carvedilol Solid Dispersion by Kneading Method. Al Mustansiriyah Journal of Pharmaceutical Sciences. 2023;23(4):367-77.

14- (USP) USP. Griseofulvin United States Pharmacopeia 43 – National Formulary 38. Rockville, MD: United States Pharmacopeial Convention; 2020. p. 3008-11.

15- Maded ZK, Sfar S, Taqa GAA, Lassoued MA, Ben Hadj Ayed O, Fawzi HA. Development and optimization of dipyridamole-and roflumilast-loaded nanoemulsion and nanoemulgel for enhanced skin permeation: formulation, characterization, and in vitro assessment. Pharmaceuticals. 2024;17(6):803.

16- Maded ZK, Lassoued MA, Taqa GAA, Fawzi HA, Abdulqader AA, Jabir MS, et al. Topical Application of Dipyridamole and Roflumilast Combination Nanoparticles Loaded Nanoemulgel for the Treatment of Psoriasis in Rats. International Journal of Nanomedicine. 2024;19:13113-34.

17- Sheth TS, Acharya F. Optimizing similarity factor of in vitro drug release profile for development of early stage formulation of drug using linear regression model. Journal of Mathematics in Industry. 2021;11(1):9.

18- Mohammed-Kadhum MF, Hameed GS. Development and characterization of furosemide-loaded binary amorphous solid dispersion to enhance solubility and dissolution for pediatric oral administration. Pharmacia. 2025;72:1-19.

19- Naamaa A. Naama , Ghaidaa S. Hameed, Dalya Basil Hanna, Mahdi ZH. Formulation of Cefdinir Ternary Solid Dispersion and Stability Study under Harsh Conditions. Al Mustansiriyah Journal of Pharmaceutical Sciences. 2025;25(1):27-48.

20- Sreeharsha N, Prasanthi S, Rao GSNK, Gajula LR, Biradar N, Goudanavar P, et al. Formulation optimization of chitosan surface coated solid lipid nanoparticles of griseofulvin: A Box-Behnken design and in vivo pharmacokinetic study. European Journal of Pharmaceutical Sciences. 2025;204:106951.

21- Kumar R, Siril PF. Preparation and characterization of polyvinyl alcohol stabilized griseofulvin nanoparticles. Materials Today: Proceedings. 2016;3(6):2261-7.

22- Al-Obaidi H, Buckton G. Evaluation of griseofulvin binary and ternary solid dispersions with HPMCAS. AAPS PharmSciTech. 2009;10(4):1172-7.

23- Ishtiaq M, Asghar S, Khan IU, Iqbal MS, Khalid SH. Development of the amorphous solid dispersion of curcumin: a rational selection of polymers for enhanced solubility and dissolution. Crystals. 2022;12(11):1606.

24- Lopez FL, Shearman GC, Gaisford S, Williams GR. Amorphous Formulations of Indomethacin and Griseofulvin Prepared by Electrospinning. Molecular Pharmaceutics. 2014;11(12):4327-38.

25- Townley ER. Griseofulvin. In: Florey K, editor. Analytical Profiles of Drug Substances. 8: Academic Press; 1979. p. 219-49.

26- Dohrn S, Reimer P, Luebbert C, Lehmkemper K, Kyeremateng SO, Degenhardt M, Sadowski G. Thermodynamic Modeling of Solvent-Impact on Phase Separation in Amorphous Solid Dispersions during Drying. Molecular Pharmaceutics. 2020;17(7):2721-33.

27- Shi Q, Chen H, Wang Y, Wang R, Xu J, Zhang C. Amorphous Solid Dispersions: Role of the Polymer and Its Importance in Physical Stability and In Vitro Performance. Pharmaceutics. 2022;14(8).

28- Sievens-Figueroa L, Pandya N, Bhakay A, Keyvan G, Michniak-Kohn B, Bilgili E, Davé RN. Using USP I and USP IV for discriminating dissolution rates of nano- and microparticle-loaded pharmaceutical strip-films. AAPS PharmSciTech. 2012;13(4):1473-82.

29- Rao VM, Lin M, Larive CK, Southard MZ. A mechanistic study of griseofulvin dissolution into surfactant solutions under laminar flow conditions. J Pharm Sci. 1997;86(10):1132-7.

30- Kumar R, Siril PF. Controlling the size and morphology of griseofulvin nanoparticles using polymeric stabilizers by evaporation-assisted solvent–antisolvent interaction method. Journal of Nanoparticle Research. 2015;17(6):256.

31- Al-Obaidi H, Petraityte I, Hibbard T, Majumder M, Kalgudi R, Zariwala MG. Antifungal nanosuspensions with surfactants and silver for the treatment of onychomycosis. European Journal of Pharmaceutics and Biopharmaceutics. 2022;179:194-205.

32- Malik B, Eman BHA-K. Formulation and in vitro /in vivo Evaluation of Silymarin Solid Dispersion- Based Topical Gel for Wound Healing. Iraqi Journal of Pharmaceutical Sciences. 2023;32(Suppl.):42-53.

33- Grover J. Methylcellulose (MC) and Hydroxypropylmethylcellulose (HPMC). 2020. p. 121-54.

34- Seftian M, Laksitorini MD, Sulaiman TNS. Drug solubility enhancement strategies using amorphous solid dispersion: Examination on type and the amount of the polymer. Indonesian Journal of Pharmaceutical Science and Technology. 2024;11(2):186-95.

35- Chella N, Daravath B, Kumar D, Tadikonda RR. Formulation and pharmacokinetic evaluation of polymeric dispersions containing valsartan. Eur J Drug Metab Pharmacokinet. 2016;41(5):517-26.

36- Budiman A, Citraloka ZG, Muchtaridi M, Sriwidodo S, Aulifa DL, Rusdin A. Inhibition of Crystal Nucleation and Growth in Aqueous Drug Solutions: Impact of Different Polymers on the Supersaturation Profiles of Amorphous Drugs—The Case of Alpha-Mangostin. Pharmaceutics. 2022;14(11):2386.

37- Wang H, Li R, Rao Y, Liu S, Hu C, Zhang Y, et al. Enhancement of the Bioavailability and Anti-Inflammatory Activity of Glycyrrhetinic Acid via Novel Soluplus®—A Glycyrrhetinic Acid Solid Dispersion. Pharmaceutics. 2022;14(9):1797.

38- Ismanelly Hanum T, Nasution A, Sumaiyah S, Bangun H. Physical stability and dissolution of ketoprofen nanosuspension formulation: Polyvinylpyrrolidone and Tween 80 as stabilizers. Pharmacia. 2023;70:209-15.

39- Wang W, Li M, Yang Q, Liu Q, Ye M, Yang G. The Opposed Effects of Polyvinylpyrrolidone K30 on Dissolution and Precipitation for Indomethacin Supersaturating Drug Delivery Systems. AAPS PharmSciTech. 2020;21(3):107.

40- Prasad R, Dalvi SV. Understanding Morphological Evolution of Griseofulvin Particles into Hierarchical Microstructures during Liquid Antisolvent Precipitation. Crystal Growth & Design. 2019;19(10):5836-49.

41- Pinto JMO, Rengifo AFC, Mendes C, Leão AF, Parize AL, Stulzer HK. Understanding the interaction between Soluplus® and biorelevant media components. Colloids and Surfaces B: Biointerfaces. 2020;187:110673.

42- Albadarin AB, Potter CB, Davis MT, Iqbal J, Korde S, Pagire S, et al. Development of stability-enhanced ternary solid dispersions via combinations of HPMCP and Soluplus® processed by hot melt extrusion. International journal of pharmaceutics. 2017;532(1):603-

43- Iemtsev A, Hassouna F, Mathers A, Klajmon M, Dendisová M, Malinová L, et al. Physical stability of hydroxypropyl methylcellulose-based amorphous solid dispersions: Experimental and computational study. International journal of pharmaceutics. 2020;589:119845.

44- Fan N, Ma P, Wang X, Li C, Zhang X, Zhang K, et al. Storage stability and solubilization ability of HPMC in curcumin amorphous solid dispersions formulated by Eudragit E100. Carbohydrate Polymers. 2018;199:492-8.

Downloads

Published

2026-06-30

How to Cite

Comparative Study of Hydrophilic Polymer-Based Solid Dispersions of Griseofulvin Incorporating HPMC E6, PVP K30, and Soluplus. (2026). Al Mustansiriyah Journal of Pharmaceutical Sciences, 26(2), 220-233. https://doi.org/10.32947/ajps.v26i2.1380

Similar Articles

51-60 of 61

You may also start an advanced similarity search for this article.

Most read articles by the same author(s)