School of Pharmaceutical Sciences, Lovely Professional University, Phagwara, India.
Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar, India.
Drug Dev Ind Pharm. 2020 Apr;46(4):597-605. doi: 10.1080/03639045.2020.1742143. Epub 2020 Mar 23.
Development of self-nanoemulsifying drug delivery systems (SNEDDS) of docosahexaenoic acid (DHA) is reported with the aim to achieve enhanced dissolution rate. The optimized composition of liquid SNEDDS (L-SNEDDS) formulation was Labrafil M1944 CS, 47% v/v Tween 80, 27% v/v Transcutol P, and 0.1% v/v DHA. L-SNEDDS were solidified using Syloid XDP 3150 as solid porous carrier. The droplet size, polydispersity index, zeta potential, percentage drug loading, and cloud point for L-SNEDDS were found to be 43.51 ± 1.36 nm, 0.186 ± 0.053, -19.20 ± 1.21 mV, 93.23 ± 1.71, and 88.60 ± 2.54 °C, respectively. Similarly, for solid SNEDDS (S-SNEDDS) the above parameters were found to be 57.32 ± 1.87 nm, 0.261 ± 0.043, -16.60 ± 2.18 mV, 91.23 ± 1.88, and 89.50 ± 1.18 °C, respectively. The formulations (L-SNEDDS, S-SNEDDS powder, and S-SNEDDS tablet) showed significant (<.05) improvement in dissolution rate of drug in 0.1 N HCl (pH 1.2) and phosphate buffer (pH 6.8) as compared to unprocessed DHA. In both the dissolution media, the dissolution rate was found more that 85% in 90 min. Absence of drug precipitation, phase separation, and turbidity during thermodynamic stability studies indicated that the developed SNEDDS were stable. Hence, it was concluded that SNEDDS have offered sufficient stability as well as dissolution rate of DHA.
报道了二十二碳六烯酸（DHA）自微乳给药系统（SNEDDS）的开发，旨在提高溶解速率。优化的液体 SNEDDS（L-SNEDDS）配方组成为 Labrafil M1944 CS、47%v/v 吐温 80、27%v/v 丙二醇、0.1%v/v DHA。L-SNEDDS 用 Syloid XDP 3150 作为固体多孔载体固化。L-SNEDDS 的粒径、多分散指数、Zeta 电位、药物载量百分比和浊点分别为 43.51 ± 1.36nm、0.186 ± 0.053、-19.20 ± 1.21mV、93.23 ± 1.71%和 88.60 ± 2.54°C。同样，对于固体 SNEDDS（S-SNEDDS），上述参数分别为 57.32 ± 1.87nm、0.261 ± 0.043、-16.60 ± 2.18mV、91.23 ± 1.88%和 89.50 ± 1.18°C。与未经处理的 DHA 相比，制剂（L-SNEDDS、S-SNEDDS 粉末和 S-SNEDDS 片剂）在 0.1N HCl（pH1.2）和磷酸盐缓冲液（pH6.8）中的药物溶解速率有显著提高（<.05）。在两种溶解介质中，90min 内的溶解速率均超过 85%。在热力学稳定性研究中，没有药物沉淀、相分离和浊度表明所开发的 SNEDDS 是稳定的。因此，结论是 SNEDDS 提供了足够的稳定性和 DHA 的溶解速率。
