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Natural Plus Synthetic Hydrotropic Solubilization using Response Surface Methodology to Optimize the Solid Dispersion
Arun Saharawat1, Deepali1, Nidhi Nainwal1
1School of Pharmaceutical Sciences and Technology, Sardar Bhagwan Singh University, Balawala, Dehradun, Uttarakhand 248001,India.
Combinatorial Chemistry & High Throughput Screening
|December 23, 2020
Summary
This study enhanced hydrochlorothiazide (HCZ) solubility using natural and synthetic hydrotropes. Blending piperazine and sodium benzoate in solid dispersions effectively improved HCZ dissolution and bioavailability.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
Background:
- Solubility and dissolution are critical for oral drug bioavailability and formulation development.
- Hydrochlorothiazide (HCZ) is a BCS Class IV drug characterized by poor solubility and permeability.
Purpose of the Study:
- To enhance the solubility and oral bioavailability of hydrochlorothiazide (HCZ).
- To investigate the efficacy of combining natural and synthetic hydrotropes for solubility enhancement.
Main Methods:
- Formulation of solid dispersions (SD) of HCZ using piperazine (natural hydrotrope) and sodium benzoate (synthetic hydrotrope).
- Optimization of HCZ solid dispersions using a 32 full factorial design.
- Evaluation of solubility and in-vitro drug release profiles.
Main Results:
- Quadratic models effectively described the relationship between hydrotrope levels and observed responses.
- Increased concentrations of both piperazine and sodium benzoate led to significant improvements in HCZ solubility.
- In-vitro drug release studies demonstrated enhanced dissolution of HCZ from the optimized solid dispersions.
Conclusions:
- The combination of natural (piperazine) and synthetic (sodium benzoate) hydrotropes offers an effective and safe strategy for enhancing hydrochlorothiazide (HCZ) solubility.
- Solid dispersion technology utilizing hydrotropes can overcome the bioavailability challenges associated with poorly soluble drugs like HCZ.
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