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Preparation and evaluation of sustained-release solid dispersions co-loading gastrodin with borneol as an oral brain-targeting enhancer.

Cai Z, Lei X, Lin Z, Zhao J, Wu F, Yang Z, Pu J, Liu Z - Acta Pharm Sin B (2014)

Bottom Line: The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form.Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced.Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.

ABSTRACT
Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain. However, stomach irritation may occur when high doses of borneol are used. In the present work, gastrodin, the main bioactive ingredient of the traditional Chinese drug "Tianma" (Rhizoma Gastrodiae) was used as a model drug to explore reasonable application of borneol. Sustained-release solid dispersions (SRSDs) for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder. The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffractometry. The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form. Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model. Subsequently, gastric mucosa irritation and the brain targeting of the SRSDs were evaluated. Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced. Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.

No MeSH data available.


Scanning electron microphotographs (500×) of gastric mucosa of rats after intragastric administration of physiological saline (A), gastrodin (B), physical mixture of gastrodin and borneol (C) and the SRSDs (D).
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f0030: Scanning electron microphotographs (500×) of gastric mucosa of rats after intragastric administration of physiological saline (A), gastrodin (B), physical mixture of gastrodin and borneol (C) and the SRSDs (D).

Mentions: The scanning electron micrographs of gastric mucosa are shown in Fig. 6. There were no abnormalities found in the gastrodin and SRSDs groups compared with the physiological saline group. However, visible gastric mucosa stripping was observed in the group treated with the physical mixture of gastrodin and borneol. The acute toxicity test dose of borneol used in this study was nearly 100 times higher than that for clinical use. In fact, the clinical gastric irritation reaction was frequently met, but not as serious as was observed in this study.


Preparation and evaluation of sustained-release solid dispersions co-loading gastrodin with borneol as an oral brain-targeting enhancer.

Cai Z, Lei X, Lin Z, Zhao J, Wu F, Yang Z, Pu J, Liu Z - Acta Pharm Sin B (2014)

Scanning electron microphotographs (500×) of gastric mucosa of rats after intragastric administration of physiological saline (A), gastrodin (B), physical mixture of gastrodin and borneol (C) and the SRSDs (D).
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4590720&req=5

f0030: Scanning electron microphotographs (500×) of gastric mucosa of rats after intragastric administration of physiological saline (A), gastrodin (B), physical mixture of gastrodin and borneol (C) and the SRSDs (D).
Mentions: The scanning electron micrographs of gastric mucosa are shown in Fig. 6. There were no abnormalities found in the gastrodin and SRSDs groups compared with the physiological saline group. However, visible gastric mucosa stripping was observed in the group treated with the physical mixture of gastrodin and borneol. The acute toxicity test dose of borneol used in this study was nearly 100 times higher than that for clinical use. In fact, the clinical gastric irritation reaction was frequently met, but not as serious as was observed in this study.

Bottom Line: The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form.Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced.Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.

View Article: PubMed Central - PubMed

Affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China.

ABSTRACT
Borneol is a traditional Chinese medicine that can promote drug absorption from the gastrointestinal tract and distribution to the brain. However, stomach irritation may occur when high doses of borneol are used. In the present work, gastrodin, the main bioactive ingredient of the traditional Chinese drug "Tianma" (Rhizoma Gastrodiae) was used as a model drug to explore reasonable application of borneol. Sustained-release solid dispersions (SRSDs) for co-loading gastrodin and borneol were prepared using ethylcellulose as a sustained release matrix and hydroxy-propyl methylcellulose as a retarder. The dispersion state of drug within the SRSDs was analyzed by using scanning electron microscopy, differential scanning calorimetry, and powder X-ray diffractometry. The results indicated that both gastrodin and borneol were molecularly dispersed in an amorphous form. Assay of in vitro drug release demonstrated that the dissolution profiles of gastrodin and borneol from the SRSDs both fitted the Higuchi model. Subsequently, gastric mucosa irritation and the brain targeting of the SRSDs were evaluated. Compared with the free mixture of gastrodin and borneol, brain targeting of SRSDs was slightly weaker (brain targeting index: 1.83 vs. 2.09), but stomach irritation obviously reduced. Sustained-release technology can be used to reduce stomach irritation caused by borneol while preserving sufficient transport capacity for oral brain-targeting drug delivery.

No MeSH data available.