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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
Published on: July 27, 2022
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Novel nanocrystal-based solid dispersion with high drug loading, enhanced dissolution, and bioavailability of
Yueqin Ma1,2, Yang Yang2, Jin Xie1
1Key Laboratory of Modern Preparation of TCM, Ministry of Education, Jiangxi University of Traditional Chinese Medicine, Nanchang, Jiangxi, 330004, ypfpharm@126.com; ypfjxutcm@126.com.
International Journal of Nanomedicine
|July 11, 2018
Summary
This study developed a quickly dissolving, high drug loading nanocrystal-based solid dispersion (NC-SD) using superdisintegrants. This novel formulation significantly enhances the oral bioavailability of poorly soluble drugs like andrographolide (AG).
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Nanotechnology
Background:
- Poorly soluble drugs often exhibit limited oral bioavailability.
- Nanocrystal-based solid dispersions (NC-SD) offer a promising approach to enhance drug dissolution.
- Optimizing dispersants is crucial for effective NC-SD formulation.
Purpose of the Study:
- To design a rapidly dissolving, high drug loading NC-SD.
- To improve the dissolution rate and oral bioavailability of poorly soluble drugs.
- To evaluate the efficacy of superdisintegrants as codispersants in AG-NC-SD.
Main Methods:
- Nanocrystal-based solid dispersions (NC-SD) were prepared using homogenization and spray-drying.
- Hydroxypropylmethylcellulose (HPMC) was used as a baseline dispersant for andrographolide (AG).
- Three superdisintegrants were evaluated as codispersants alongside HPMC, mannitol, and lactose.
Main Results:
- Superdisintegrants, particularly sodium carboxymethyl starch, significantly enhanced AG-NC-SD dissolution and redispersion via swelling-triggered mechanisms.
- A formulation with 15% sodium carboxymethyl starch, 15% HPMC, and 10% lactose achieved high drug loading (67.83%) and fast dissolution.
- The optimized AG-NC-SD demonstrated significantly improved in vivo oral bioavailability compared to coarse AG.
Conclusions:
- A surfactant-free NC-SD with high drug load and rapid dissolution can be successfully prepared using superdisintegrants as codispersants.
- This formulation strategy offers a feasible method for enhancing the oral bioavailability of poorly soluble drugs.
- Superdisintegrant-enhanced NC-SD represents a significant advancement in oral drug delivery.
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