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新型喷雾干燥聚合物粒子用于控制肺部药物传递的特性研究。

Characterization of novel spray-dried polymeric particles for controlled pulmonary drug delivery.

机构信息

Department of Pharmaceutics and Biopharmacy, Philipps-Universität, Ketzerbach 63, D-35037 Marburg, Germany.

出版信息

J Control Release. 2012 Mar 10;158(2):329-35. doi: 10.1016/j.jconrel.2011.10.030. Epub 2011 Oct 29.

Abstract

Numerous studies have addressed the controlled pulmonary drug delivery properties of colloidal particles. However, only scant information on the potential of spray-drying for submicron particle preparation is available. By exploiting the advantages of spray-drying, the characteristics of submicron particles can be optimized to meet the requirements necessary for lung application. Submicron particles were prepared from organic poly(d,l-lactide-co-glycolide) (PLGA) solutions, and composite particles were spray-dried from aqueous PLGA nanosuspensions. The feed concentration, as well as the spray-mesh diameter influenced the resulting particle sizes. Nanoparticles were virtually unaffected after spray-drying. The aerodynamic characteristics of both particle species revealed aerosol particle sizes suitable for deposition in the deep lungs (≤4μm). While the entrapped drug was released within 90min from the composite particles, extensive drug retardation (480min) was observed for PLGA particles spray-dried from organic solution. These results suggest that nanospray-drying is a convenient method to prepare submicron, controlled drug delivery vehicles useful for pulmonary application potentially allowing access to alveolar tissue.

摘要

许多研究都涉及胶体颗粒的受控肺部药物传递特性。然而,关于喷雾干燥在亚微米颗粒制备方面的潜力的信息却很少。通过利用喷雾干燥的优势,可以优化亚微米颗粒的特性,以满足肺部应用所需的要求。亚微米颗粒是从有机聚(D,L-丙交酯-共-乙交酯)(PLGA)溶液中制备的,复合颗粒是从水性 PLGA 纳米混悬液中喷雾干燥得到的。进料浓度以及喷雾网眼直径影响所得颗粒尺寸。喷雾干燥后,纳米颗粒几乎没有受到影响。这两种颗粒的空气动力学特性均揭示了适合沉积在肺部深处(≤4μm)的气溶胶颗粒尺寸。虽然复合颗粒中的包埋药物在约 90min 内释放,但从有机溶液中喷雾干燥的 PLGA 颗粒中观察到药物的广泛延迟(~480min)。这些结果表明,纳米喷雾干燥是一种制备亚微米控制药物释放载体的简便方法,可用于肺部应用,可能使肺泡组织得以进入。

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