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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.


In vitro dissolution profiles of gastrodin and borneol from the physical mixture of drugs with excipients and the SRSDs (n=6).
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f0025: In vitro dissolution profiles of gastrodin and borneol from the physical mixture of drugs with excipients and the SRSDs (n=6).

Mentions: The mean cumulative release of gastrodin and borneol with time is shown in Fig. 5. The SRSDs were able to sustain drugs release for 8 h. The release rate of gastrodin was higher than that of borneol, because gastrodin is readily soluble in water. Indeed, more than 60% of gastrodin was released within 2 h. These SRSDs in powder show significant sustained-release effect compared to crude drugs. They could be reformulated for oral dosage (tablets, capsules and pills) that might provide better control of drug release rate.


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)

In vitro dissolution profiles of gastrodin and borneol from the physical mixture of drugs with excipients and the SRSDs (n=6).
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0025: In vitro dissolution profiles of gastrodin and borneol from the physical mixture of drugs with excipients and the SRSDs (n=6).
Mentions: The mean cumulative release of gastrodin and borneol with time is shown in Fig. 5. The SRSDs were able to sustain drugs release for 8 h. The release rate of gastrodin was higher than that of borneol, because gastrodin is readily soluble in water. Indeed, more than 60% of gastrodin was released within 2 h. These SRSDs in powder show significant sustained-release effect compared to crude drugs. They could be reformulated for oral dosage (tablets, capsules and pills) that might provide better control of drug release rate.

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.