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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.


Powder X-ray patterns of gastrodin (A), borneol (B), EC+HPMC (C), physical mixture of drugs with EC and HPMC (D) and the SRSDs (E).
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f0020: Powder X-ray patterns of gastrodin (A), borneol (B), EC+HPMC (C), physical mixture of drugs with EC and HPMC (D) and the SRSDs (E).

Mentions: The PXRD pattern of pure borneol indicated that borneol was crystalline as demonstrated by several distinctive peaks observed at 2θ of 13.92°, 15.11°, and 16.18° (Fig. 4B). Moreover, the physical mixture of drugs and excipients showed the same series of three peaks. In contrast, all these characteristic peaks of borneol were absent in the diffraction spectrum of the SRSDs, suggesting that borneol was not in crystalline form. These findings demonstrated that both gastrodin and borneol in the SRSDs were molecularly dispersed in an amorphous form, thus confirming the formation of solid dispersions.


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)

Powder X-ray patterns of gastrodin (A), borneol (B), EC+HPMC (C), physical mixture of drugs with EC and HPMC (D) and the SRSDs (E).
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0020: Powder X-ray patterns of gastrodin (A), borneol (B), EC+HPMC (C), physical mixture of drugs with EC and HPMC (D) and the SRSDs (E).
Mentions: The PXRD pattern of pure borneol indicated that borneol was crystalline as demonstrated by several distinctive peaks observed at 2θ of 13.92°, 15.11°, and 16.18° (Fig. 4B). Moreover, the physical mixture of drugs and excipients showed the same series of three peaks. In contrast, all these characteristic peaks of borneol were absent in the diffraction spectrum of the SRSDs, suggesting that borneol was not in crystalline form. These findings demonstrated that both gastrodin and borneol in the SRSDs were molecularly dispersed in an amorphous form, thus confirming the formation of solid dispersions.

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.