Abstract
Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, however, realizing the controlled drug release behavior of a hot-melt blended medicament it is still a tough challenge. In this study, we developed a simple and effective heat treatment method to adjust the drug release behavior, without the addition of any release modifiers. Thin metoprolol tartrate (MPT)/poly(ε-caprolactone) (PCL) tablets were prepared through hot-melt processing, and different morphologies of MPT were obtained by altering processing temperatures and the following heat treatment. MPT particles with different particle sizes were obtained under different processing temperatures, and fibrous crystals of MPT were fabricated during the following heat treatment. Different morphological structures of MPT adjusted the drug diffusion channel when immersed in phosphate-buffered saline (PBS), and various drug release behaviors were approached. After being immersed for 24 h, 7% of the MPT was released from the blend processed at 130 °C, while more than 95% of the MPT were released after the following heat treatment of the same sample. Thus, flexible drug release behaviors were achieved using this simple and effective processing manufacture, which is demonstrated to be of profound importance for biomedical applications.
Highlights
Published: 13 September 2021Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, by virtue of the advantages such as solvent-free, continuous, and efficient processing [1,2,3]
The Hansen solubility parameters of the compounds were calculated from the chemical structure using the approaches of Hoftyzer and van Krevelen [22,23,24,25]
The pure PCL exhibited a melting temperature of 63.6 ◦ C, which is in accordance with the results reported elsewhere [36]
Summary
Published: 13 September 2021Hot-melt blending has been widely used in the pharmaceutical industry to produce drug delivery systems, by virtue of the advantages such as solvent-free, continuous, and efficient processing [1,2,3]. With the development of clinical medicine, a drug delivery system is often required to achieve controlled drug release in order to maintain a stable blood drug concentration, reduce the side effects of drugs, and achieve a high therapeutic effect. Realizing the controlled drug release behavior of a hot-melt blended medicament is still a tough challenge. Numerous attempts have been made to adjust the drug release behavior of hot-melt blended medicaments, mostly focusing on the selection of polymer matrix and the interaction between polymer matrix and loaded drug. The drug release behavior is subject to three aspects: the water solubility of the loaded drug, the permeability of the drug through the polymer matrix, and the biodegradability of the polymer matrix [10]
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