da Silveira Walteçá Louis Lima, Damasceno Bolivar P G L, Ferreira Laura F, Ribeiro Izabel L S, Silva Karolyne S, Silva André Leandro, Giannini Maria José Mendes, da Silva-Júnior Arnóbio Antônio, de Oliveira Anselmo Gomes, do Egito E Sócrates Tabosa
Department of Pharmacy, Universidade Federal do Rio Grande do Norte, Rua Praia de Areia Branca, 8948, CEP 59094-450, Natal, RN, Brazil.
Curr Drug Deliv. 2016;13(6):982-93. doi: 10.2174/1570159x14666151109110734.
Amphotericin B eye drops are widely used in the treatment of ocular infections. However, amphotericin's toxicity leads to low patient compliance and aggravation of symptoms. This work describes the development of a microemulsion system containing amphotericin B, aiming for its use in ocular applications.
The microemulsion was developed by the titration technique. The physicochemical characteristics were determined with both loaded and unloaded amphotericin B-microemulsion. The nanostructures were analyzed by polarized light microscopy. The microdilution method was used to establish the minimum inhibitory concentration against fungal strains, and, therefore, evaluate the microemulsion activity. Additionally, in order to evaluate the microemulsion toxicity an in vitro toxicity assay against red blood cells was performed.
The performed studies showed that the presence of amphotericin B loaded into the system did not induce serious changes in the physicochemical properties of the microemulsion when compared to the unloaded system. The spectrophotometric studies depicted amphotericin B-self-associated species, which allow predicting its behavior in vitro. The high pressure liquid chromatography results revealed high drug content entrapment in the microemulsion droplet. Finally, the amphotericin B-microemulsion in vitro susceptibility test showed high activity against Candida strains and a low toxicity profile against red blood cells when compared to Fungizone®.
The physicochemical characterization of the microemulsion demonstrated that its characteristics are compatible with the topical ocular route, making it eligible for consideration as a new and interesting amphotericin B-deliverydosage form to be used as eye drop formulation.
两性霉素B滴眼液广泛用于眼部感染的治疗。然而，两性霉素的毒性导致患者依从性低且症状加重。本研究描述了一种含两性霉素B的微乳系统的研发，旨在将其用于眼部应用。
通过滴定技术制备微乳。对载有和未载两性霉素B的微乳进行理化特性测定。用偏光显微镜分析纳米结构。采用微量稀释法确定对真菌菌株的最低抑菌浓度，从而评估微乳的活性。此外，为评估微乳的毒性，进行了针对红细胞的体外毒性试验。
所进行的研究表明，与未载药系统相比，载有两性霉素B的系统的存在并未引起微乳理化性质的严重变化。分光光度研究描绘了两性霉素B的自缔合物种，这有助于预测其体外行为。高压液相色谱结果显示微乳滴中药物含量高。最后，与两性霉素B脂质体相比，两性霉素B微乳的体外药敏试验显示对念珠菌菌株具有高活性，对红细胞的毒性较低。
微乳的理化特性表明其特性与眼部局部给药途径相容，使其有资格被视为一种新型且有趣的两性霉素B给药剂型，用作滴眼液制剂。
