Improvement in oral bioavailability and dissolution of tanshinone IIA by preparation of solid dispersions with porous silica

Abstract

SDs with porous silica as carrier could achieve superior oral bioavailability by improving drug dissolution, whereas drug stability could be maintained.

Design and pharmaceutical applications of porous particles

“…37 Sylysia 350, a common type of PSi, with pore size at 21.0 nm and pore volume at 1.6 mL g À1 , has many silanol groups on its surface and can be applied as a pharmaceutical excipient for oral administration because of its good biocompatibility, stability, and nontoxicity. 7,53 In addition, it has an excellent capacity to improve the powder properties and the dissolution of drugs. Therefore, PSi is widely used as a carrier to enhance various properties of drugs in pharmaceutical eld.…”

“…Recently, there are many literatures reported that PSi combined with the SD technology (PSi-SD) achieved preferable solubilization of drugs. 7,[53][54][55] For example, Yan et al 7 reported that tanshinone IIA (tanIIA) in PSi-SD with different ratios (1 : 2 to 1 : 8) showed signicantly improved dissolution rates ($4-fold at maximum) compared to pure tanIIA and corresponding physical mixtures. Besides, the AUC 0-24 h of tanIIA from PSi-SD increased by 1.97 times compared with pure tanIIA, demonstrating that its oral bioavailability was improved by SD with PSi.…”

“…Meanwhile, the formation of hydrogen bonds could improve the wettability of the drug and further increase drug dissolution rates. 7,57 On the other hand, the enhancement of dissolution seems to be negatively affected by drug loading. 58 PSi can improve the tableting properties of powders.…”

“…For example, when a drug is loaded into the pores of PPs, it tends to keep in an amorphous state. 7 Nano-connement can also happen when the pore size of PPs is nano-scaled. 90 Moreover, large surface area, high porosity, and suitable pore size of PPs can facilitate water inltration into the inner of PPs and thus increase the contact area between dissolution media and drug.…”

“…[1][2][3][4] As part of the effort, porous particles (PPs) based on old pharmaceutical materials emerged and have been developed as a novel carrier to improve drug delivery, dissolution, tableting, and so on. [5][6][7] PPs are low-density solids with open or closed pore structures that provide a large exposed surface area. 8 Originated in the twentieth century, they have been used in various elds, and especially in the pharmaceutical eld signicant results have been achieved.…”