Preparation and Evaluation of Glaucocalyxin A Sustained- Release Pellets Based on Phospholipid Complex System with Enhanced Bioavailability

Objective: Glaucocalyxin A (GLA) suffers from low oral bioavailability and rapid in vivo metabolism. Therefore, the purpose of this study was to develop a new formulation to enhance the oral bioavailability simultaneously sustained release of GLA.

Material and methods: GLA-phospholipid complex was firstly formulated by solvent-evaporation method to improve the solubility of GLA. Differential scanning calorimetry, powder X-ray diffraction, scanning electron microscopy, and solubility study were used to characterize the GLA-phospholipid complex. And then, the optimized GLA-phospholipid complex was selected to prepare GLA-phospholipid complex sustained release pellets by extrusion-spheronization and fluidized bed coating technology. The prepared pellets were studied by in vitro drug release study and administered to beagle dogs to evaluate the oral bioavailability of GLA-phospholipid complex and GLA-phospholipid complex sustained release pellets.

Results: The results illustrated that GLA in GLA-phospholipid complex was either molecularly dispersed or in an amorphous form with 13.8- fold water solubility than the free GLA. The pharmacokinetic studies in beagle dogs demonstrated that GLA-phospholipid complex and GLA-phospholipid complex sustained-release pellets showed 2.19-fold and 2.07-fold improvement than the free GLA by oral dosage, respectively. Further, steady plasma concentration, and prolonger Tmax were simultaneously obtained from GLA-phospholipid complex sustained release pellet.

Conclusion: These outcomes suggested that the combination of phospholipid complex and sustained release pellets could enhance the oral bioavailability and prolong the action time in vivo which provided a promising delivery system for GLA.

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Article information: Miao YF, Sun JQ. Preparation and Evaluation of Glaucocalyxin A Sustained-Release Pellets Based on Phospholipid Complex System with Enhanced Bioavailability. J Pharmaceu Pharmacol. 2020; 8(1): 7.

Materials: Glaucocalyxin A was obtained from College of Pharmaceutical Science, Soochow University (Suzhou, China). Lipoid E80 (trade name of phospholipid)was purchased from Shanghai Dongshang BiologyTechnique Ltd. (Shanghai, China). Lactose was purchased from Meggle. (Germany). Kollicoat SR 30 D was purchased from BASF (Germany). Unless otherwise stated, all other materials were of analytical grade.