“DEVELOPMENT AND OPTIMIZATION OF DANAZOL CO-CRYSTAL LOADED TABLET TO TREAT ENDOMETRIOSIS”

Vidya A. Patil, Shivraj Jadhav, Sunil Mahajan
In: Prospects in Pharmaceutical Sciences · 2025 · doi:10.56782/pps.525 · W4416832120
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⚙ AI-generated summary by claude@2026-06, 2026-06-09 ⓘ

Danazol-malonic acid co-crystals in optimized tablets showed enhanced solubility, rapid disintegration, and improved dissolution compared to the marketed formulation for endometriosis treatment.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-09 · read from full text ⓘ

The paper studied the development, optimization, and characterization of danazol co-crystal–loaded tablets intended to enhance danazol solubility and dissolution for endometriosis treatment. Danazol co-crystals were produced by solvent evaporation using different co-formers and characterized by FTIR, DSC, and XRD, then formulated into tablets via direct compression with optimization using a 3² factorial design varying sodium croscarmellose and PVP K-30; disintegration, dissolution, physical parameters, and accelerated stability were assessed. The danazol–malonic acid co-crystal (1:2) produced the largest solubility increase (about 13.8-fold) with evidence of a new crystalline phase by XRD, and the optimized tablet formulation (VF7) showed faster disintegration and higher dissolution than the marketed product while remaining stable for three months under accelerated conditions. This paper is centrally about endometriosis — it develops danazol co-crystal tablets to improve drug solubility and dissolution for treating endometriosis.

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Abstract

This study aimed to develop, optimize, and characterize Danazol co-crystal-loaded tablets to enhance solubility and dissolution, thereby improving therapeutic efficacy in the treatment of endometriosis. Danazol co-crystals were prepared using various pharmaceutically acceptable co-formers via the solvent evaporation method and characterized using Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Among the systems studied, Danazol-malonic acid co-crystals (1:2 molar ratio) demonstrated the greatest solubility enhancement (11.42 ± 0.53 μg/mL), corresponding to a 13.76-fold increase compared to pure Danazol. The formation of a novel crystalline phase was confirmed by distinct XRD peaks at 2θ values of 19° and 21°. Co-crystals were incorporated into tablets using direct compression and optimized using a 3² factorial design, with sodium croscarmellose (8–24 mg) and polyvinylpyrrolidone K-30 (4–20 mg) as independent variables. The formulations were assessed for pre-compression characteristics, tablet quality parameters, disintegration time, in vitro drug release, and stability. Statistical analysis revealed strong predictive models for disintegration time (R² = 0.9971) and drug release (R² = 0.9483). The optimized formulation (VF7) containing 24 mg sodium croscarmellose and 4 mg PVP K-30 exhibited rapid disintegration (74.0 ± 3.2 s) and significantly improved dissolution (95.8 ± 2.0% at 60 min), outperforming the marketed formulation (75.2 ± 2.7%). The optimized tablets remained stable under accelerated conditions (40°C/75% RH) for three months. These findings highlight the potential of co-crystallization and formulation optimization to overcome solubility challenges, offering a promising strategy for improving the clinical performance of Danazol in endometriosis therapy.
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Objectives

To develop, optimize, and characterize danazol co-crystal-loaded tablets for enhanced solubility and dissolution in order to improve therapeutic efficacy in endometriosis treatment. Methods: Danazol co-crystals were prepared using various co-formers through a solvent evaporation technique and characterized by FTIR, DSC, and XRD. Co-crystals were formulated into tablets using direct compression and optimized through a 3² factorial design, varying sodium croscarmellose (8—24 mg) and PVP K-30 (4—20 mg) concentrations. Formulations were evaluated for pre-compression properties, physical parameters, disintegration, dissolution, and stability. Results: Danazol-malonic acid co-crystals (1:2 ratio) exhibited the highest solubility enhancement (11.42 ± 0.53 μg/mL, 13.76-fold increase). XRD confirmed the formation of a new crystalline phase with distinct peaks at 19° and 21° 2θ. The quadratic models for both disintegration time (R² = 0.9971) and drug release (R² = 0.9483) demonstrated excellent predictive capability. Formulation VF7 (24 mg sodium croscarmellose, 4 mg PVP K-30) was identified as optimal with rapid disintegration (74.0 ± 3.2 seconds) and superior dissolution (83.6 ± 3.4% at 30 minutes, 95.8 ± 2.0% at 60 minutes) compared to the marketed product (75.2 ± 2.7% at 60 minutes). The optimized formulation maintained stability under accelerated conditions (40°C/75% RH) for three months. Conclusion: The optimized danazol co-crystal tablet formulation successfully overcame the solubility and dissolution limitations of this poorly soluble drug, potentially enhancing bioavailability and therapeutic efficacy while reducing dosing frequency for endometriosis patients. This approach presents a promising platform for improving clinical outcomes and patient compliance in endometriosis management. - Lucky Vasave, Shivraj Jadhav, Rushikesh Bachhav, Sunil Mahajan, Deepak Sonawane, Formulation and evaluation of gastro-retentive in-situ gel of anti-ulcer drug misoprostol , Prospects in Pharmaceutical Sciences: Vol. 23 No. 4 (2025) - Rushikesh Mahale, Shivraj Jadhav, Sunil Mahajan, Development and optimization of gastro retentive floating tablets of dapsone for controlled release , Prospects in Pharmaceutical Sciences: Vol. 24 No. 1 (2026) - Rama Devi Korni, Thanmaisree Bora, Akhil Majji, Jagadeesh Panda, Liquisolid technique for solubility enhancement of a poorly soluble thrombin inhibitor: optimization using design of experiments and artificial neural networks , Prospects in Pharmaceutical Sciences: Vol. 23 No. 3 (2025) - Dr. Ashwini Madgulkar, Dr. Mangesh Bhalekar, Abhishek Kunjir, Maryam Mulla, A SCIENTIFIC EXPLORATION OF CO-AMORPHOUS FORMULATION DRIVEN BY KNOWLEDGE BASED VIRTUAL SCREENING FOR SOLUBILITY AND BIOAVAILABILITY ENHANCEMENT OF DARUNAVIR , Prospects in Pharmaceutical Sciences: Early Access (ONLINE FIRST) - Vijayraj Sonawane, Dhanashree I. Wagh, Sakshi P. Bhamare, Khemchand R. Surana, Deepak D. Sonawane, Sunil K. Mahajan, Enhancing water solubility of a BCS Class II drug using hydrotropy, mixed solvency, co-solvency, and nanosuspension techniques , Prospects in Pharmaceutical Sciences: Vol. 23 No. 4 (2025) - Monika Nijhawan, Bhavana Jidige, Rajeswari Aleti, Sailaja Gunnam, Trapti Saxena, Development and characterization of voriconazole-oxalic acid dihydrate cocrystals for enhanced pharmaceutical performance , Prospects in Pharmaceutical Sciences: Vol. 22 No. 4 (2024) - 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) - 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: Vol. 24 No. 1 (2026) - Rushikesh Mahale, Shivraj Jadhav, Sunil Mahajan, Development and optimization of gastro retentive floating tablets of dapsone for controlled release , Prospects in Pharmaceutical Sciences: Vol. 24 No. 1 (2026) - Ewa Napiórkowska, Overview of cyclodextrins and medicinal products containing cyclodextrins currently registered in Poland , Prospects in Pharmaceutical Sciences: Vol. 21 No. 3 (2023) - 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) - Bartłomiej Pyrak, Tomasz Gubica, Karolina Rogacka-Pyrak, Cyclodextrin nanosponges as bioenhancers of phytochemicals , Prospects in Pharmaceutical Sciences: Vol. 22 No. 3 (2024) You may also start an advanced similarity search for this article. Details

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Statistics Authors Citation rules Patil, V., Jadhav, S., & Mahajan, S. (2025). Development and optimization of danazol co-crystal loaded tablet to treat endometriosis. Prospects in Pharmaceutical Sciences, 23(4), 220–234. https://doi.org/10.56782/pps.525 Licence This work is licensed under a Creative Commons Attribution 4.0 International License.

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