通过使用Penetratin用于眼科悬浮剂提高角质药物透率
Ryo Morofuji1,2, Kazuhiro Kudo1,2, Takahiro Honda2
1Division of Materials Science, Nara Institute of Science and Technology.
Biological & pharmaceutical bulletin
|May 26, 2024
概括
透 (PNT) 是一种细胞透的,增强了眼科悬浮中的药物吸收. 在一个ex vivo模型中,最佳PNT度改善了角膜药物递送,显示了改善眼睛治疗的潜力.
科学领域:
- 眼科医生 眼科 眼科
- 生物技术是生物技术.
- 药物运输 药物运输 药物运输
背景情况:
- 眼科悬浮剂面临药物生物可用性和颗粒相关问题的挑战.
- 提高生物可用性对于降低药物度和相关风险至关重要.
- 目前,用于眼科药物输送的有效透增强剂的数量有限.
研究的目的:
- 为了研究透 (PNT) 的潜力,一个细胞透 (CPP),作为透增强剂在眼科悬浮剂.
- 评估PNT对角膜药物吸收的影响及其在改善眼科药物输送中的适用性.
主要方法:
- 在实验室中使用重建的人类角膜上皮组织模型 (LabCyte CORNEA-MODEL24) 进行角膜吸收研究.
- 猪眼睛模型,以评估PNT对雷巴米皮德眼科悬浮剂的影响.
- 使用MTT测定进行细胞毒性评估,并评估各种pH值的储存稳定性.
主要成果:
- 在没有共价结合的体外角膜模型中,PNT增强了微球的吸收.
- 在一个ex vivo模型中,10μM PNT显著改善了悬浮中的rebamipide的角膜吸收.
- 100μM PNT 的较高度是无效的,可能是由于粒子聚合.
结论:
- 佩内特拉丁作为眼科悬浮剂的透增强剂显示出希望.
- 优化PNT度可以改善角膜药物输送,可能导致更有效的眼科治疗.
- 需要进一步的研究来确定最佳的PNT度和配方条件.
相关概念视频
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
129
Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...
129
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
198
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
198
01:22Drug Delivery: Miscellaneous Routes
338
Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection, and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
338
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
807
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
807
01:27Factors Influencing Drug Absorption: Drug Dissolution
467
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
467
01:25Routes of Drug Administration: Parenteral
1.9K
The administration of drugs via parenteral routes allows for direct drug introduction into the systemic circulation, resulting in high bioavailability because the medication bypasses the harsh conditions of the gastrointestinal tract and hepatic metabolism.
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
The intravenous route (IV) of drug administration can be further categorized into two types. The bolus injection administers the entire dose rapidly, while an intravenous infusion slowly delivers smaller doses steadily.
The IV route is often...
1.9K