采用 33 全因子设计,研究眼部兼容脂质和蓖麻油对酒石酸溴莫尼定纳米乳液制备的影响。

IF 4.2 Q3 Pharmacology, Toxicology and Pharmaceutics Recent patents on inflammation & allergy drug discovery Pub Date : 2018-01-01 DOI:10.2174/1872213X12666180730115225
Rimple, Maria J Newton
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引用次数: 10

摘要

背景:酒石酸溴莫尼定(BRT酒石酸溴莫尼定(BRT)用于治疗青光眼。本研究工作制备了酒石酸溴莫尼定纳米乳液,以提高其通过屏障的渗透性,加快起效和治疗效果:通过使用表面活性剂和辅助表面活性剂,制备眼部兼容的酒石酸溴莫尼定纳米乳液:方法:实验工作包括利用傅立叶变换红外光谱(FTIR)、电化学稳定性分析(DSC)和X射线衍射(XRD)进行相容性研究和结晶度研究。用马尔文 S90 光子相关光谱仪对制备的纳米乳液进行粒度分析,并对 Z 平均值(d.nm.)和 PDI 进行表征。此外,还利用激光光散射技术和 TEM 进行了进一步研究:研究表明,制剂 BN2、BN3 和 BN10 的 Z 平均值分别为 19.48、22.14 和 26.50 d.nm。在 PDI 分别为 0.337、0.270、0.289 的情况下,配方 BN2、BN3、BN10 的分布平均直径(nm)分别为 376.8 + 258.4、542.8 + 494.4、398.8 + 263.9,直径分别为 267.5、298.5、272.7。BN10 的 zeta 电位为 -21.26 mV,其他参数如 TEM 和药物释放研究也有报道:结论:使用蓖麻油、Lipoid S75(含 70% 磷脂酰胆碱的无脂大豆磷脂)、Lipoid E80(含 80% 磷脂酰胆碱的鸡蛋磷脂)和 PF- 68 成功制备了酒石酸溴莫尼定纳米乳剂。优化配方显示出较低的液滴尺寸、令人满意的 zeta 电位、较高的药物载量和可重复的药物释放曲线。Brimonidne taratarate 在最近的多项专利中都有不同的应用,是未来治疗的潜在候选药物。纳米乳液作为传统眼科制剂的潜在替代品,受到了广泛的关注。它通过减少药物蛋白结合、增加角膜驻留时间、提高药物渗透性和提供持续的药物释放来提高眼部生物利用度。
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Impact of Ocular Compatible Lipoids and Castor Oil in Fabrication of Brimonidine Tartrate Nanoemulsions by 33 Full Factorial Design.

Background: Brimonidine Tartrate (BRT) is used in the treatment of glaucoma. Brimonidine tartrate nanoemulsion was fabricated in this research work to enhance the permeability through barriers and faster onset of action and therapeutic effect.

Objective: To fabricate an ocular compatible nanoemulsion of brimonidine tartrate by using surfactant and co-surfactants.

Methods: The experimental work involved compatibility studies by using FTIR, DSC and crystallinity study by XRD. The prepared nanoemulsion was studied by photon correlation spectroscopy by Malvern S90 for the particle size analysis and characterized for Z average value (d.nm.) and PDI. Further studies were conducted by laser light scattering technique by delsanano common and TEM.

Results: The study demonstrated that the formulations BN2, BN3, BN10 demonstrated the z average value of 19.48, 22.14,26.50 d.nm. With 0.337, 0.270, 0.289 PDI respectively, the formulae BN2, BN3, BN10 demonstrated the distribution average diameter (nm) of 376.8 + 258.4, 542.8 + 494.4, 398.8 + 263.9 with the diameter of 267.5, 298.5, 272.7, respectively. The zeta potential of BN10 was -21.26 mV and other parameters such as TEM and drug release studies were also reported.

Conclusion: The nanoemulsion of brimonidine tartrate was prepared successfully by using castor oil, Lipoid S75 (Fat free soybean phospholipids with 70% phosphatidylcholine), Lipoid E80 (Egg phospholipids with 80% phosphatidylcholine) and PF- 68. The optimised formula demonstrated the lower droplet size, satisfactory zeta potential, and high drug loading and reproducible drug release profile. Brimonididne taratarate is reported in various recent patents for various applications and is the potential candidate for future therapy. Nanoemulsion is widely explored as potential alternatives for conventional ophthalmic formulation based approaches. It enhances the ocular bioavailability by reducing the drug protein binding, increasing the corneal resident time, enhancing the drug permeability and providing a sustained drug release.It reported a significant increase in therapeutic efficacy for various chronic ocular disease states of both the anterior and posterior ocular segments.

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期刊介绍: Recent Patents on Inflammation & Allergy Drug Discovery publishes review articles by experts on recent patents in the field of inflammation and allergy drug discovery e.g. on novel bioactive compounds, analogs and targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in inflammation and allergy drug design and discovery.
期刊最新文献
Meet Our Editorial Board Member Diagnosis of Allergic Reactions to Drugs Non-steroidal Anti-inflammatory Drugs Other Antimicrobial Drugs Biologics: Monoclonal Antibodies for Non-cancer Therapy, Cytokines, Fusion Proteins, Enzymes, and Hormones
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