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Determination of Alteration in Micromeritic Properties of a Solid Dispersion: Brunauer-Emmett-Teller Based Adsorption
Lovepreet Singh1, Lakhvir Kaur2, Gurjeet Singh1
1Department of Pharmaceutics, Khalsa College of Pharmacy, Amritsar, Punjab, 143001, India.
Abstract:
The present study is focused on the use of solid dispersion technology to triumph over the solubility-related problems of bexarotene which is currently used for treating various types of cancer and has shown potential inhibitory action on COVID-19 main protease and human ACE2 receptors. It is based on comparison of green locust bean gum and synthetic poloxamer as polymers using extensive mechanistic methods to explore the mechanism behind solubility enhancement and to find suitable concentration of drug to polymer ratio to prepare porous 3rd generation solid dispersion. The prepared solid dispersions were characterized using different studies like X-ray diffraction (XRD), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM), Brunauer-Emmett-Teller (BET), differential scanning calorimetry (DSC), and particle size analysis in order to determine the exact changes occurred in the product which are responsible for enhancing solubility profiles of an insoluble drug. The results showed different profiles for particle size, solubility, dissolution rate, porosity, BET, and Langmuir specific surface area of prepared solid dispersions by using different polymers. In addition to the comparison of polymers, the BET analysis deeply explored the changes occurred in all dispersions when the concentration of polymer was increased. The optimized solid dispersion prepared with MLBG using lyophilization technique showed reduced particle size of 745.7±4.4 nm, utmost solubility of 63.97%, pore size of 211.597 Å, BET and Langmuir specific surface area of 5.6413 m2/g and 8.2757 m2/g, respectively.
Insights
This study enhances bexarotene solubility using solid dispersion technology with green locust bean gum. Optimized formulations show improved particle size, solubility, and surface area for cancer and potential COVID-19 treatments.
Area of Science:
- Pharmaceutical Technology
- Materials Science
Background:
- Bexarotene is an anti-cancer drug with poor solubility, limiting its efficacy.
- Bexarotene exhibits potential inhibitory action against COVID-19 targets (main protease and ACE2 receptors).
- Solid dispersion technology offers a promising approach to overcome poor drug solubility.
Purpose of the Study:
- To enhance the solubility and dissolution rate of bexarotene using solid dispersion.
- To compare the efficacy of green locust bean gum (MLBG) and poloxamer as polymers for bexarotene solid dispersions.
- To investigate the mechanism of solubility enhancement and optimize drug-to-polymer ratios.
Main Methods:
- Preparation of bexarotene solid dispersions using lyophilization with MLBG and poloxamer.
- Characterization using XRD, TGA, SEM, DSC, particle size analysis, BET, and Langmuir surface area analysis.
- Evaluation of solubility, dissolution rate, porosity, and specific surface area.
Main Results:
- Optimized solid dispersion with MLBG showed significantly reduced particle size (745.7±4.4 nm) and enhanced solubility (63.97%).
- MLBG-based dispersion exhibited improved pore size (211.597 Å) and surface area (BET: 5.6413 m²/g, Langmuir: 8.2757 m²/g).
- BET analysis elucidated the impact of polymer concentration on dispersion characteristics.
Conclusions:
- Green locust bean gum is an effective polymer for creating porous bexarotene solid dispersions with enhanced solubility.
- Solid dispersion technology, particularly with MLBG, offers a viable strategy to improve bexarotene's pharmaceutical profile.
- The findings support further development of bexarotene solid dispersions for therapeutic applications, including potential antiviral uses.
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