Abstract
The active ingredients of salvia (dried root of Salvia miltiorrhiza) include both lipophilic (e.g., tanshinone IIA, tanshinone I, cryptotanshinone and dihydrotanshinone I) and hydrophilic (e.g., danshensu and salvianolic acid B) constituents. The low oral bioavailability of these constituents may limit their efficacy. A solid self-microemulsifying drug delivery system (S-SMEDDS) was developed to load the various active constituents of salvia into a single drug delivery system and improve their oral bioavailability. A prototype SMEDDS was designed using solubility studies and phase diagram construction, and characterized by self-emulsification performance, stability, morphology, droplet size, polydispersity index and zeta potential. Furthermore, the S-SMEDDS was prepared by dispersing liquid SMEDDS containing liposoluble extract into a solution containing aqueous extract and hydrophilic polymer, and then freeze-drying. In vitro release of tanshinone IIA, salvianolic acid B, cryptotanshinone and danshensu from the S-SMEDDS was examined, showing approximately 60%–80% of each active component was released from the S-SMEDDS in vitro within 20 min. In vivo bioavailability of these four constituents indicated that the S-SMEDDS showed superior in vivo oral absorption to a drug suspension after oral administration in rats. It can be concluded that the novel S-SMEDDS developed in this study increased the dissolution rate and improved the oral bioavailability of both lipophilic and hydrophilic constituents of salvia. Thus, the S-SMEDDS can be regarded as a promising new method by which to deliver salvia extract, and potentially other multicomponent drugs, by the oral route.
Highlights
Salvia is the dried root or rhizome of Salvia miltiorrhiza Bunge, which is part of the Labiatae family of flowering plants
The active ingredients of salvia can be divided into two major groups (Figure 1): lipophilic diterpenoid quinone constituents, including tanshinone IIA, tanshinone I, cryptotanshinone and dihydrotanshinone I; and hydrophilic phenolic acid compounds, including danshensu, salvianolic acid B and protocatechuic aldehyde [1]
Considering the formulations oxidation of lipidhydrophilic components drugs duringcould storage), well asvery possible issues and risks of of leakage the formulations filled hard gelatin. To address such critical and self-microemulsifying drug delivery systems (SMEDDS), it when has other drawbacks,are such as into a smaller rangecapsules of dosage forms, low manageability challenge, we report a solid(owing self-microemulsifying delivery between system that developed and/or to portability, andhere a limited shelf-life to problems ofdrug interactions thewas constituents oxidation of lipid components during storage), as well as possible compatibility issues and risks of leakage when the formulations are filled into hard gelatin capsules [19,20]. To address such critical challenge, here we report a solid self-microemulsifying drug delivery system that was developed to allow the various constituents of salvia to be loaded into a single drug delivery system and improve the oral bioavailability of both hydrophilic and hydrophobic compounds
Summary
Salvia is the dried root or rhizome of Salvia miltiorrhiza Bunge, which is part of the Labiatae family of flowering plants. To address such critical and SMEDDS, it when has other drawbacks,are such as into a smaller rangecapsules of dosage forms, low manageability challenge, we report a solid(owing self-microemulsifying delivery between system that developed and/or to portability, andhere a limited shelf-life to problems ofdrug interactions thewas constituents oxidation of lipid components during storage), as well as possible compatibility issues and risks of leakage when the formulations are filled into hard gelatin capsules [19,20] To address such critical challenge, here we report a solid self-microemulsifying drug delivery system that was developed to allow the various constituents of salvia to be loaded into a single drug delivery system and improve the oral bioavailability of both hydrophilic and hydrophobic compounds. The drug release characteristics and bioavailability of the novel S-SMEDDS were assessed
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