Departamento de Odontologia, Universidade Ibirapuera, Av. Interlagos 1329 - 4° andar, São Paulo, SP, 04661-100, Brazil.
Faculdade de Odontologia, Universidade Santo Amaro, Av. Prof. Eneas de Siqueira Neto, 340, São Paulo, SP, 04829-900, Brazil.
AAPS PharmSciTech. 2023 Feb 9;24(2):56. doi: 10.1208/s12249-023-02517-8.
Chitosan particles loaded with dibasic calcium phosphate anhydrous (DCPA) is a promising strategy for combining antimicrobial and osteoconduction properties in regenerative medicine. However, mostly micrometer-sized particles have been reported in the literature, limiting their use and reducing their effect in the biomedical field. We have recently overcome this limitation by developing submicrometer-sized particles with electrospray technique. The objective of this study was to understand how the process parameters control the size and properties of submicrometer chitosan particles loaded with DCPA. Solutions of 10 mg/mL chitosan and 2.5 mg/mL DCPA in a 90% acetic acid were electrosprayed under three distinct flow rate conditions: 0.2, 0.5, and 1.0 mL/h. The particles were crosslinked in a glutaraldehyde atmosphere and characterized in terms of their morphology, inorganic content, zeta potential, and minimum inhibitory concentration (MIC) against S. mutans. All conditions showed particles with two similar morphologies: one small-sized with a spherical shape and another larger-sized with a bi-concave shape. All generated a broad particle size distribution, with a similar mean size of ~ 235 nm. The addition of DCPA decreased the zeta potential for all the samples, but it was above 30 mV, indicating a low aggregation potential. The lower flow rate showed the worst efficacy for DCPA incorporation. Antimicrobial activity was greater in chitosan/DCPA particles with flow rate of 0.5 mL/h. It can be concluded that the flow rate of 0.5 mL/h presents the best compromise solution in terms of morphology, zeta potential, MIC, and inorganic content.
载二水合磷酸氢钙(DCPA)的壳聚糖颗粒是将抗菌和骨传导性能结合在再生医学中的一种很有前途的策略。然而,文献中大多报道的是微米级颗粒,限制了它们的使用并降低了它们在生物医学领域的效果。我们最近通过使用电喷雾技术开发出了亚微米级颗粒克服了这一限制。本研究的目的是了解过程参数如何控制载 DCPA 的亚微米壳聚糖颗粒的大小和性能。将 10mg/mL 壳聚糖和 2.5mg/mL DCPA 的溶液在三种不同流速条件下(0.2、0.5 和 1.0mL/h)进行电喷雾。将颗粒在戊二醛气氛中交联,并根据其形态、无机含量、Zeta 电位和最小抑菌浓度(MIC)对变异链球菌的抑制作用进行表征。所有条件下的颗粒都具有两种相似的形态:一种是小尺寸的球形,另一种是较大尺寸的双凹形。所有条件下生成的颗粒均具有相似的宽粒径分布,平均粒径约为 235nm。DCPA 的加入降低了所有样品的 Zeta 电位,但仍高于 30mV,表明聚集潜力较低。较低的流速对 DCPA 的掺入效果最差。在流速为 0.5mL/h 的壳聚糖/DCPA 颗粒中表现出更强的抗菌活性。可以得出结论,流速为 0.5mL/h 在形态、Zeta 电位、MIC 和无机含量方面呈现出最佳的折衷解决方案。