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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.


Chemical structures of borneol (A) and gastrodin (B).
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f0005: Chemical structures of borneol (A) and gastrodin (B).

Mentions: In many compounds employed in traditional Chinese medicine (TCM), a so-called messenger drug is usually included. It is capable of introducing the main effective drugs in the prescription to the target site to increase therapeutic efficacy1–3. The bicyclic monoterpene borneol (Fig. 1A) is one such messenger drug that is frequently used in the treatment of encephalopathy like stroke, epilepsy and headache. Studies have shown that borneol can promote drug absorption from the gastrointestinal tract and facilitate distribution to the brain4–8. However, stomach irritation may occur when a high dose of borneol is used9,10, which limits the clinical application of borneol as an oral brain-targeting enhancer.


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)

Chemical structures of borneol (A) and gastrodin (B).
© Copyright Policy - CC BY-NC-ND
Related In: Results  -  Collection

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

f0005: Chemical structures of borneol (A) and gastrodin (B).
Mentions: In many compounds employed in traditional Chinese medicine (TCM), a so-called messenger drug is usually included. It is capable of introducing the main effective drugs in the prescription to the target site to increase therapeutic efficacy1–3. The bicyclic monoterpene borneol (Fig. 1A) is one such messenger drug that is frequently used in the treatment of encephalopathy like stroke, epilepsy and headache. Studies have shown that borneol can promote drug absorption from the gastrointestinal tract and facilitate distribution to the brain4–8. However, stomach irritation may occur when a high dose of borneol is used9,10, which limits the clinical application of borneol as an oral brain-targeting enhancer.

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.