Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra, India.
Bharati Vidyapeeth College of Pharmacy, Kolhapur 416013, Maharashtra, India.
J Pharm Sci. 2021 Jan;110(1):280-291. doi: 10.1016/j.xphs.2020.10.020. Epub 2020 Oct 15.
In this investigation, the fabrication of capsaicin loaded self nano emulsifying drug delivery system (SNEDDS) was attempted to improve the effectiveness of capsaicin through the oral route. A pseudo-ternary phase diagram was constructed at different km values (1:1, 2:1, & 3:1). Nine liquid formulations (L-CAP-1 to L-CAP-9) were prepared at km = 3, evaluated & converted to solid free-flowing granules using neusilin® US2. L-CAP-3 comprising of 15% isopropyl myristate, 33.75% Labrafil, & 11.25% ethanol exhibited higher % transmittance (98.90 ± 1.24%) & lower self-emulsification time (18.19 ± 0.46 s). FT-IR spectra showed no incompatibility whereas virtual analysis confirmed hydrogen bond interaction between amino hydrogen in the capsaicin & oxygen of the neusilin. DSC & XRD study revealed the amorphization & molecular dispersion of capsaicin in S-SNEDDS. TEM analysis confirmed the nano-sized spherical globules. Within 15 min, L-SNEDDS, S-SNEDDS, & pure capsaicin showed 87.36 ± 3.25%, 85.19 ± 4.87%, & 16.61 ± 3.64% drug release respectively. S-CAP-3 significantly (P < 0.001) inhibited the proliferation of HT-29 colorectal cancer cells than capsaicin. Apoptosis assay involving Annexin V/PI staining for S-CAP-3 treated cells demonstrated a significant (P < 0.001) apoptotic rate. Remarkably, 3.6 fold increase in bioavailability was observed after oral administration of capsaicin-SNEDDS than plain capsaicin.
在这项研究中，尝试通过口服途径来提高辣椒素的功效，将辣椒素负载自纳米乳化药物传递系统 (SNEDDS) 制成。在不同的 km 值 (1:1、2:1 和 3:1) 下构建伪三元相图。在 km = 3 下制备了 9 种液体配方 (L-CAP-1 至 L-CAP-9)，进行了评估并使用 Neusilin® US2 转化为自由流动的固体颗粒。包含 15%异丙基肉豆蔻酸、33.75%Labrafil 和 11.25%乙醇的 L-CAP-3 表现出更高的透光率（98.90 ± 1.24%）和更低的自乳化时间（18.19 ± 0.46 s）。FT-IR 光谱显示没有不相容性，而虚拟分析证实了辣椒素中的氨基氢与 Neusilin 之间的氢键相互作用。DSC 和 XRD 研究表明，在 S-SNEDDS 中辣椒素呈非晶态和分子分散。TEM 分析证实了纳米尺寸的球形液滴。在 15 分钟内，L-SNEDDS、S-SNEDDS 和纯辣椒素分别显示 87.36 ± 3.25%、85.19 ± 4.87%和 16.61 ± 3.64%的药物释放。与辣椒素相比，S-CAP-3 显著（P < 0.001）抑制 HT-29 结直肠癌细胞的增殖。用 Annexin V/PI 染色进行的 S-CAP-3 处理细胞的凋亡试验显示出显著的（P < 0.001）凋亡率。值得注意的是，与普通辣椒素相比，口服给予辣椒素-SNEDDS 后生物利用度显著提高了 3.6 倍。
