Application of NMP and Neusilin US2-integrated liquisolid technique in mini-tablets for improving the physical performances and oral bioavailability of liposoluble supercritical fluid extracts
Frankincense and myrrh are widely used Chinese medicines, showing clinically relevant synergistic therapeutic effects in the treatment of inflammation and cancer. We investigated the applicability of a liquisolid (LS) technique to the preparation of mini-tablets containing supercritical fluid extracts of frankincense and myrrh (SFE-FM) to improve oral bioavailability of their active compounds. Nine drug-loaded liquisolid formulations (LS-A to LS-I) were prepared based on a mathematical model, and the powder properties of the formulations were determined. Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) were used for evaluation of the physicochemical properties of SFE-FM in the liquisolid formulations.
In addition, mini-tablet’s tensile strength, disintegration time, tablet mechanical property, stability, in vitro dissolution rate, and in vivo pharmacokinetic were measured. The results showed that the contact angle of the SFE-FM was significantly lower with N-methyl-2-pyrrolidone (NMP) than with Tween 80; the liquisolid powder formed with NMP exhibited excellent flowability. Moreover, owing to its superior compressibility, Neusilin US2 was found to be more suitable as a coating material than the commonly used Aerosil 200. The release of active compounds was significantly better when mini-tablets containing SFE-FM were prepared with the liquisolid technique, compared with that from traditional mini-tablets.
The AUC(0–t) of the active compounds, including 3-acetyl-11-keto-beta-boswellic acid (AKBA), β-elemonic acid, and β-boswellic acid (β-BA) in the LS-B mini-tablet was 1.33, 1.84, and 1.52 times higher than that of a traditional mini-tablet, respectively (P < 0.05). Thus, the liquisolid compression technique represents a promising approach for enhancing the dissolution performance and oral bioavailability of liquid liposoluble drugs, including SFE-FM.
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Wansi Li, Yongtai Zhang, Panwen Huang, Ying Liu, Yongjia Zhang, Zhi Wang, Nianping Feng, Application of NMP and Neusilin US2-integrated liquisolid technique in mini-tablets for improving the physical performances and oral bioavailability of liposoluble supercritical fluid extracts, Journal of Drug Delivery Science and Technology, Volume 81, 2023, 104205, ISSN 1773-2247, https://doi.org/10.1016/j.jddst.2023.104205.