English
Liquisolid technique for solubility enhancement of a poorly soluble thrombin inhibitor: optimization using design of experiments and artificial neural networks
Rama Devi Korni
Thanmaisree Bora
Akhil Majji
Jagadeesh Panda
Abstract
The current work uses liquisolid (LS) technology to increase the absorption efficiency and dissolution rate of the weakly water-soluble drug dabigatran etexilate (DE) by formulating it using the design of experiments (DoE) and comparing it with the artificial neural network (ANN). D-optimal design in Stat-Ease software was used to formulate and optimize DE liquisolid capsules. The drug-to-nonvolatile solvent ratio (X1 – 25 to 50), carrier-to-coating ratio (X2 – 10 to 30), type of nonvolatile solvent (X3 – PEG 400 or Kolliphor EL) and type of carrier (X4 – Neusilin or Fujicalin) were taken as independent variables and percentage drug release (Y1) and angle of repose (Y2) were taken as dependent variables. The results were compared to artificial neural networks (ANN) utilizing JMP software to improve the prediction of the chosen output variables. The optimized formulation was developed and evaluated. The R2 value of the D-optimal design for percentage drug release was 0.914, whereas for ANN, it was 0.943. The mean square error (MSE) value of the quadratic model obtained in the D-optimal design was 90.76, and in ANN, it was only 2.392. The R2 value for the quadratic model in the D-optimal design for the angle of repose was 0.723, whereas for ANN, it was 0.751. The MSE for the D‑optimal design was 28.11, whereas for ANN, it was 11.04. Based on the analysis of results, PEG400 was selected as the nonvolatile solvent and Neusilin as a carrier for optimized formulation. The percentage drug release and angle of repose of optimized DE liquisolid capsules were found to be 86.23 ± 1.37 and 36.08 ± 0.63, respectively. XRD studies indicated a reduction in the crystallinity of the drug in liquisolid formulations. The findings suggested that dabigatran etexilate's solubility rate could be increased by using liquisolid capsules. ANN gave better predictability than the design of experiments.
Keywords:
Liquisolid, design of experiments, D-optimal design, artificial neural networks, JMPSimilar Articles
- monika nijhawan, Rajeswari Aleti, Sravani Maramwar, Dedipya Goda Srivalli Vangala, Trapti Saxena, Solubility Enhancement of Diacerein Through Liquisolid Technology: A Formulation Perspective , Prospects in Pharmaceutical Sciences: No. 2025 (Early Access)
- Priya Jagtap, Dr. Reshma Jadhav, Dr. Ashish Jain, Bhavesh Mahajan, Prapti Gawand, Prathamesh Chaudhari, Aishwarya Patil, Quality by design approach in HPLC method development and validation for simultaneous determination of abiraterone acetate and prednisolone with greenness assessment , Prospects in Pharmaceutical Sciences: Vol. 23 No. 3 (2025)
- Sailaja Gunnam, Sindhura T, Rajeswari Aleti, Monika Nijhawan, Bi-layer tablets of sitagliptin phosphate & metformin hydrochloride – preparation and evaluation , Prospects in Pharmaceutical Sciences: Vol. 23 No. 3 (2025)
- Komal Parmar, Rishi Bharatia, Novel flucytosine loaded in-situ gel for the management of ocular infections , Prospects in Pharmaceutical Sciences: Vol. 23 No. 3 (2025)
- Rushikesh Mahale, Shivraj Jadhav, Sunil Mahajan, Development and optimization of gastro retentive floating tablets of dapsone for controlled release , Prospects in Pharmaceutical Sciences: No. 2025 (Early Access)
- Sylwia Kraczkowska, Zofia Suchocka, Jan Pachecka, ELEVATED BLOOD LEVEL OF HOMOCYSTEINE AS INDICATOR OF HEALTH HAZARD , Prospects in Pharmaceutical Sciences: Vol. 3 No. 3 (2005)
- Monika Pawłowska, DESIGN AND PROPERTIES ANALYSIS OF MOLECULARLY IMPRINTED POLYMERS. MOLECULAR MODELING METHOD APPLICATION , Prospects in Pharmaceutical Sciences: Vol. 10 No. 2 (2012)
- Ewa Napiórkowska, Overview of cyclodextrins and medicinal products containing cyclodextrins currently registered in Poland , Prospects in Pharmaceutical Sciences: Vol. 21 No. 3 (2023)
- Piotr Bojanowski, Piotr F. J. Lipiński, Paweł Czekała, Dariusz Plewczyński, MULTITARGET DRUGS – A NEW PARADIGM IN DRUG DESIGN , Prospects in Pharmaceutical Sciences: Vol. 11 No. 1 (2013)
- Agnieszka Lis-Cieplak, ADAMANTANE DERIVATIVES - VARIETY OF BIOLOGICAL ACTIVITIES. A REVIEW OF MEDICATIONS APPROVED IN POLAND AND POTENTIAL DRUGS , Prospects in Pharmaceutical Sciences: Vol. 10 No. 3 (2012)
You may also start an advanced similarity search for this article.
Details
References
Statistics
Authors
Citation rules
Cited by / Share
Licence
This work is licensed under a Creative Commons Attribution 4.0 International License.