通过实验设计开发和优化达沙替尼的超饱和自纳米乳化给药系统

Q2 Pharmacology, Toxicology and Pharmaceutics International Journal of Applied Pharmaceutics Pub Date : 2024-05-07 DOI:10.22159/ijap.2024v16i3.50434
C. Rajinikanth, K. Kathiresan
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引用次数: 0

摘要

研究目的本研究配制了自纳米乳化超饱和给药系统 S-SNEDDS,以获得优异的药物溶解性和稳定性:方法:利用饱和溶解度,使用 capryol ® 90、cremophor®-EL 和 transcutol HP 制成 S-SNEDDS。利用三元相图对其组成进行了优化。采用响应面方法的中心复合设计,达沙替尼-SNEDDS 对液滴大小(Y1)、多分散指数(Y2)和 15 分钟内药物释放率(Y3)产生了响应。在优化的 SNEDDS(S3)中添加了各种沉淀抑制剂,以制成 S-SNEDDS 并进行评估:最佳配方为 S3,粒径为 128 nm,zeta 电位为 21 mV。甲基纤维素的过饱和度优于其他抑制剂。优化制剂(F3)的zeta电位(-25 mV)更高,粒径(128 nm)更小,因此比普通SNEDDS更稳定。差示扫描量热法和 X 射线粉末衍射显示达沙替尼在 S-SNEDDS 中为无定形。F3的90分钟释放率(>99%)高于纯药物分散体(26%)和SNEDDS制剂(95%):结果表明,S-SNEDDS制剂成功地提高了达沙替尼的溶解度和稳定性。
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DEVELOPMENT AND OPTIMIZATION OF SUPER SATURABLE SELF-NANO EMULSIFYING DRUG DELIVERY SYSTEM FOR DASATINIB BY DESIGN OF EXPERIMENT
Objective: In current research, Self-Nanoemulsifying Super Saturable Drug Delivery Systems S‑SNEDDS was formulated to attain superior drug dissolution and stability. Methods: Using saturated solubility, capryol ® 90, cremophor®-EL, and transcutol HP were used to make S-SNEDDS. Its composition was optimized using the ternary phase diagram. Using the central composite design of Response Surface Methodology, dasatinib-SNEDDS developed responses for droplet size (Y1), polydispersity index (Y2), and % drug released in 15 min (Y3). Various Precipitation Inhibitors were added to optimize SNEDDS (S3) to make S-SNEDDS and evaluate. Results: The optimum formulation was S3, with a particle size of 128 nm and zeta potential of-21 mV. Methylcellulose was shown better supersaturation than other inhibitors. The optimized formulation (F3) was more stable than ordinary SNEDDS due to its more significant zeta potential (-25 mV) and lower particle size (128 nm). Dasatinib was shown to be amorphous in S-SNEDDS using Differential Scanning Calorimetry and X-ray Powder Diffraction. F3 had a higher 90 min release rate (>99%) than pure drug dispersion (26%) and SNEDDS formulation (95%). Conclusion: The results concluded that S-SNEDDS formulation successfully enhanced the dissolution and stability of dasatinib.
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来源期刊
International Journal of Applied Pharmaceutics
International Journal of Applied Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
CiteScore
1.40
自引率
0.00%
发文量
219
期刊介绍: International Journal of Applied Pharmaceutics (Int J App Pharm) is a peer-reviewed, bimonthly (onward March 2017) open access journal devoted to the excellence and research in the pure pharmaceutics. This Journal publishes original research work that contributes significantly to further the scientific knowledge in conventional dosage forms, formulation development and characterization, controlled and novel drug delivery, biopharmaceutics, pharmacokinetics, molecular drug design, polymer-based drug delivery, nanotechnology, nanocarrier based drug delivery, novel routes and modes of delivery; responsive delivery systems, prodrug design, development and characterization of the targeted drug delivery systems, ligand carrier interactions etc. However, the other areas which are related to the pharmaceutics are also entertained includes physical pharmacy and API (active pharmaceutical ingredients) analysis. The Journal publishes original research work either as a Original Article or as a Short Communication. Review Articles on a current topic in the said fields are also considered for publication in the Journal.
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