Solubility enhancement of diacerein through liquisolid technology: a formulation perspective
DOI:
https://doi.org/10.56782/pps.477Keywords:
liquisolid compacts, Diacerein, Solubility enhancement, poorly aqueous soluble, formulation developmentAbstract
Liquisolid systems present an effective technique for improving the dissolution rate and oral bioavailability of poorly water-soluble drugs. The objective of this study is to formulate and evaluate diacerein liquisolid compacts using Tween 80 as the liquid vehicle, Neusilin and Fujicalin as carriers, and Aerosil 200 as a coating material. Sodium starch glycolate and magnesium stearate were used as disintegrants and lubricants, respectively. Pre- and post-compression parameters such as flow properties, hardness, friability, drug content, and disintegration time were measured. The in vitro release characteristics of the pure drug, marketed capsules (as reference), and liquisolid technique (test sample) were studied. Among all the formulations, FSC3 had the highest dissolving efficiency (DE) of 53.109% at 60 minutes, exceeding the marketed product's DE of 44.972%. FTIR analysis revealed no drug-excipient incompatibility, and all tested formulations fulfilled pharmacopeial requirements for flow and mechanical characteristics. Overall, the study demonstrates that the liquisolid technique significantly improves the dissolution of diacerein, indicating its potential to boost the physicochemical properties of poorly soluble drugs.
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1. Kumari, L.; Choudhari, Y.; Patel, P.; Gupta, GD.; Singh, D.; Rosenholm, J.M.; Bansal, K.K.; Kurmi, B.D. Advancement in Solubilization Approaches: A Step towards Bioavailability Enhancement of Poorly Soluble Drugs. Life 2023, 13(5), Art. No: 1099. DOI: 10.3390/life13051099 DOI: https://doi.org/10.3390/life13051099
2. Kumar; H.; Rajpoot. A.K.; Sharma, S.; Kumar, A. Solid Lipid Nanoparticles: A Strategy to Improve Oral Delivery of the Biopharmaceutics Classification System (BCS) Class II Drugs. Int. J. Pharm. Biol. Sci. Arch. 2018, 9(4), 204-215.
3. Eltobshi, A.A.; Mohamed, E.A.; Abdelghani, G.M.; Nouh, A.T. Self-nanoemulsifying drug-delivery systems for potentiated anti-inflammatory activity of diacerein. Int. J. Nanomed. 2018, 13, 6585-6602. DOI: 10.2147/IJN.S178819 DOI: https://doi.org/10.2147/IJN.S178819
4. Premakumar, SV.; B. A, Vishwanath.; Deepthi Swapna. Enhancement of Solubility and Dissolution Rate of BCS Class II Drugs. Int. J. Pharm. Sci. Rev. Res. 2024, 84(7), 153-161. DOI: 10.47583/ijpsrr.2024.v84i07.023 DOI: https://doi.org/10.47583/ijpsrr.2024.v84i07.023
5. Talekar, S.; Dave, R. Solubility enhancement of a BCS class II drug using granulated fumed silica as an adsorbent. J. Pharm. Res. Int. 2017, 18(6), Art. No: JPRI.36872. DOI: 10.9734/JPRI/2017/36872 DOI: https://doi.org/10.9734/JPRI/2017/36872
6. Kumar Nagabandi, V.; Ramarao, T.; Jayaveera, K.N. Liquisolid compacts: a novel approach to enhance bioavailability of poorly soluble drugs. Int. J. Pharm. Biol. Sci. 2011, 1(3), 89-102.
7. Dias, RJ.; Mali, KK.; Ghorpade, VS.; Havaldar, VD.; Mohite, VR. Formulation and evaluation of carbamazepine liquisolid compacts using novel carriers. Indian. J. Pharm. Educ. Res. 2017, 51(S2), S69-78. DOI: 10.5530/ijper.51.2s.52 DOI: https://doi.org/10.5530/ijper.51.2s.52
8. Nijhawan, M.; Santhosh, A.; Babu, PR.; Subrahmanyam, CV. Solid state manipulation of lornoxicam for cocrystals--physicochemical characterization. Drug. Dev. Ind. Pharm. 2013, 40(9), 1163-1172. DOI: 10.1590/s2175 97902022e191024 DOI: https://doi.org/10.3109/03639045.2013.804834
9. Suryawanshi, V.K.; Gidwani, B.; Verma, A.; Dubey, N.; Kaur, C.D. Formulation and evaluation of ramipril liquisolid compact using novel carrier. Int. J. Pharm. Sci. Res. 2019, 10(2), 917-25. DOI: 10.13040/IJPSR.0975-8232 DOI: https://doi.org/10.13040/IJPSR.0975-8232
10. Wankhede Navneet, B.; Walekar, S. S.; Sadgir, P.S.; Ahirrao, S.P. Liquisolid: A Novel Technique for Dissolution Enhancement of Poorly Water-Soluble Drugs. Asian J. Pharm. Technol. Innov. 2014, 2(8), 77-90.
11. El-Hammadi, M.; Awad, N. Investigating the use of liquisolid compacts technique to minimize the influence of pH variations on loratadine release. AAPS PharmSciTech. 2012, 13(1), 53-58. DOi: 10.1208/s12249-011-9719-6 DOI: https://doi.org/10.1208/s12249-011-9719-6
12. Patel, G.K.; Patel, J. Formulation and evaluation of liquisolid compacts of rivaroxaban. Int. J. Emerg. Technol. Innov. Res. 2022, 9(7), e152-e162
13. Spireas, S.; Bolton, M. Liquisolid systems and methods of preparing same. (Patent No: 6,423,339). United States Patent. 2002. Available at: https://patents.google.com/patent/US6423339B1/en (Accessed on 11 February 2025)
14. Sai, P.D.; Sivaiah, K.V.; Bonthagarala, B.; Rao, P.V. Review on liquisolid compact technology. World. J. Pharm. Res. 2014, 4, 293-306.
15. Nijhawan, M.; Godugu, M.; Saxena, T.; Farheen, T.; Dwivedi, K. Pharmaceutical co-crystals of posaconazole for improvement of physicochemical properties. Braz. J. Pharm. Sci. 2022, 58, Art. No: e191024. DOI: 10.1590/s2175 97902022e191024 DOI: https://doi.org/10.1590/s2175-97902022e191024
16. Andrew E.C et al. Formulation and in Vitro Evaluation of Liquisolid Compact of Celecoxib. Mathews J. Pharm. Sci. 2024, 8(2), Art. No: 31. DOI: 10.30654/MJPS.10031 DOI: https://doi.org/10.30654/MJPS.10031
17. Patel, U.B.; Modi, D.C.; Shah, D.P. Liquisolid compacts: A review. Int. J. Adv. Pharm. 2017, 6(7), 110-3.
18. Madhavi Harika Srimathkandala, Sushma M, Madhu Babu Ananthula, Vasudha Bakshi. Formulation and evaluation of Loperamide Liquisolid compacts. Int. J. Pharm. 2016, 6(2), 93-99.
19., Costa, P.; Sousa Lobo, J.M.. Modeling and comparison of dissolution profiles, Eur. J. Pharm. Sci. 2001, 13(2), 123-133. DOI: 10.1016/s0928-0987(01)00095-1 DOI: https://doi.org/10.1016/S0928-0987(01)00095-1
20. Kassaye, L.; Genete, G. Evaluation and comparison of in-vitro dissolution profiles for different brands of amoxicillin capsules. Afr. Health. Sci. 2013, 13(2), 369-375. DOI: 10.4314/ahs.v13i2.25 DOI: https://doi.org/10.4314/ahs.v13i2.25
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