Abstract

This study investigates the effects of direct and indirect dispersion methods for lovastatin solid dispersion (LSD) in alginate (AG)/chitosan (CS) composites on the characteristics and properties of the AG/CS/LSD composites. The preparation method significantly influences the structure, morphology, and LSD size distribution of the composites as well as the drug release of LSD from the samples. The differences in dispersion methods for LSD lead to differences in the interaction between the components, the structure, and the control drug release of LSD. Lovastatin was released from the samples containing LSD in two stages (a fast release stage and a slow release stage), and the drug release content prepared using the indirect method is lower than that prepared using the direct method in the same buffer solution. After 32 h of testing, the released LSD content from the indirect and direct LSD dispersion methods in pH 2 and pH 7.4 buffer solutions was 87–94% and 41–61%, respectively. Drug release kinetics from the above samples in solutions with different pH values was also set up.

Highlights

  • Lovastatin, a natural product with a potential inhibitory e ect on HMG-CoA reductase, was synthesized in 1979 and rst applied in medicine in 1987

  • It is worth noting that the morphology of LVS had changed in terms of size and shape owing to variations in face dimensions or the appearance/disappearance of some crystal faces [23]. e size of LVS in the D-lovastatin solid dispersion (LSD) samples decreased after loading to the AG/CS composites. e LVS was coated by polymers; we did not observe any appearance of LVS bars in the structures of the D-LSD samples. is can be attributed to the formation of hydrogen bonds and electrical interactions between hydroxyl, amine, and carbonyl groups of AG and CS with hydroxyl and carbonyl groups of LVS

  • For the ID-LSD1 and ID-LSD2 samples, the LVS became bar shaped with size ranging from 500 to 3000 nm. e surface of the LVS bars was coated by a thin AG film

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Summary

Introduction

Lovastatin, a natural product with a potential inhibitory e ect on HMG-CoA reductase, was synthesized in 1979 and rst applied in medicine in 1987. It is absorbed rapidly in the small intestine if administered orally. E plasma concentration of lovastatin reaches its maximum within 4 h. It has a short half-life of 3 h and a low bioavailability of 5% [1]. E authors showed methanol and acetone to be suitable solvents for the preparation of lovastatin nanocrystal, at 3 mM concentration of drug. Basavaraj et al used nanotechnology to reduce the particle size of lovastatin from micron size to nanosize level by precipitation process without the use of surfactants or stabilizers [2]. e authors showed methanol and acetone to be suitable solvents for the preparation of lovastatin nanocrystal, at 3 mM concentration of drug. e dissolution rate of nanocrystal drug in methanol and acetone was doubled due to the contact of the drug particles with a larger

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