Pešić Nikola, Ivković Branka, Barudžija Tanja, Grujić Branka, Ibrić Svetlana, Medarević Djordje
Department of Pharmaceutical Technology and Cosmetology, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Pharmaceutics. 2024 Dec 24;17(1):6. doi: 10.3390/pharmaceutics17010006.
BACKGROUND/OBJECTIVES: Selective laser sintering (SLS) is one of the most promising 3D printing techniques for pharmaceutical applications as it offers numerous advantages, such as suitability to work with already approved pharmaceutical excipients, the elimination of solvents, and the ability to produce fast-dissolving, porous dosage forms with high drug loading. When the powder mixture is exposed to elevated temperatures during SLS printing, the active ingredients can be converted from the crystalline to the amorphous state, which can be used as a strategy to improve the dissolution rate and bioavailability of poorly soluble drugs. This study investigates the potential application of SLS 3D printing for the fabrication of tablets containing the poorly soluble drug carvedilol with the aim of improving the dissolution rate of the drug by forming an amorphous form through the printing process.
Using SLS 3D printing, eight tablet formulations were produced using two different powder mixtures and four combinations of experimental conditions, followed by physicochemical characterization and dissolution testing.
Physicochemical characterization revealed that at least partial amorphization of carvedilol occurred during the printing process. Although variations in process parameters were minimal, higher temperatures in combination with lower laser speeds appeared to facilitate a greater degree of amorphization. Ultimately, the partial conversion to the amorphous form significantly improved the dissolution of carvedilol compared to its pure crystalline form.
Obtained results suggest that the SLS 3D printing technique can be effectively used to convert poorly water-soluble drugs to their amorphous state, thereby improving solubility and bioavailability.
背景/目的：选择性激光烧结（SLS）是用于药物应用的最具前景的3D打印技术之一，因为它具有许多优点，例如适合与已批准的药用辅料一起使用、无需使用溶剂以及能够生产具有高载药量的快速溶解的多孔剂型。当粉末混合物在SLS打印过程中暴露于高温时，活性成分可从结晶态转变为非晶态，这可作为提高难溶性药物溶出速率和生物利用度的一种策略。本研究调查了SLS 3D打印在制备含有难溶性药物卡维地洛的片剂方面的潜在应用，目的是通过打印过程形成非晶态来提高药物的溶出速率。
使用SLS 3D打印，采用两种不同的粉末混合物和四种实验条件组合制备了八种片剂配方，随后进行了物理化学表征和溶出度测试。
物理化学表征表明，在打印过程中卡维地洛至少发生了部分非晶化。尽管工艺参数的变化很小，但较高的温度与较低的激光速度相结合似乎有助于更大程度的非晶化。最终，与纯结晶形式相比，部分转变为非晶态显著改善了卡维地洛的溶出度。
所得结果表明，SLS 3D打印技术可有效地用于将难水溶性药物转变为非晶态，从而提高溶解度和生物利用度。
