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Enhanced Brain targeting delivery of Salvianic Acid using Borneol as a promoter of Blood/Brain transport and regulator of P-gp
- Source :
- Current Drug Delivery. 20
- Publication Year :
- 2023
- Publisher :
- Bentham Science Publishers Ltd., 2023.
-
Abstract
- Background: Borneol can enhance the blood-brain barrier (BBB) permeability of some drugs and suppress the efflux transport of P-glycoprotein (P-gp), which will contribute to the brain delivery of salvianic acid A (SAA). Objective: The study aimed to develop an approach to improve the brain targeting delivery of SAA with the aid of borneol. Methods: “Borneol” was involved in SAA via esterified prodrug SAA borneol ester (SBE) and combined administration (SAA-borneol, SAA-B). Subsequently, the blood-brain transport of SAA through brain/blood distribution and P-gp regulation via expression and function assay were investigated in rats. Results: The SBE and SAA-B-treated group received a three-fold brain concentration and longer t1/2 and retention period of active SAA than that of SAA alone (20.18/13.82 min vs. 6.48 min; 18.30/17.42 min vs. 11.46 min). In addition, blood to brain transport of active SAA in SBE was altered in comparison to that of SAA-B, ultimately resulting in a better drug targeting index (9.93 vs. 3.63). Further studies revealed that SBE-induced downregulation of P-gp expression occurred at the later stage of administration (60 min, P < 0.01), but SBE always showed a more powerful drug transport activity across BBB represented by Kp value of rhodamine 123 than SAA-B (30, 60 min, P < 0.05). Conclusion: The comparative results indicate that SBE exhibits prominent efficiency on SAA's targeting delivery through improved blood/brain metabolic properties and sustained inhibitory effect of “borneol” on P-gp efflux. Therefore, prodrug modification can be applied as a more effective approach for brain delivery of SAA.
- Subjects :
- Pharmaceutical Science
Subjects
Details
- ISSN :
- 15672018
- Volume :
- 20
- Database :
- OpenAIRE
- Journal :
- Current Drug Delivery
- Accession number :
- edsair.doi...........cbfb038f68e1e8e8fa69b10eb02ebd82