Characteristics of Microparticles Based on Resorbable Polyhydroxyalkanoates Loaded with Antibacterial and Cytostatic Drugs

Abstract

The development of controlled drug delivery systems, in the form of microparticles, is an important area of experimental pharmacology. The success of the design and the quality of the obtained microparticles are determined by the method of manufacture and the properties of the material used as a carrier. The goal is to obtain and characterize microparticles depending on their method of preparation, the chemical composition of the polymer and the load of the drugs. To obtain microparticles, four types of degradable PHAs, differing in their chemical compositions, degrees of crystallinity, molecular weights and temperature characteristics, were used (poly-3-hydroxybutyrate and copolymers 3-hydroxybutyric-co-3-hydroxyvaleric acid, 3-hydroxybutyric-co-4-hydroxybutyric acid, and 3-hydroxybutyric-co-3-hydroxyhexanoic acid). The characteristics of microparticles from PHAs were studied. Good-quality particles with an average particle diameter from 0.8 to 65.0 μm, having satisfactory ζ potential values (from −18 to −50 mV), were obtained. The drug loading content, encapsulation efficiency and in vitro release were characterized. Composite microparticles based on PHAs with additives of polyethylene glycol and polylactide-co-glycolide, and loaded with ceftriaxone and 5-fluorouracil, showed antibacterial and antitumor effects in E. coli and HeLa cultures. The results indicate the high potential of PHAs for the design of modern and efficient drug delivery systems.

Recent Advances in the Therapeutic Potential of Carotenoids in Preventing and Managing Metabolic Disorders

“…Microstructures range from 1 to 1000 μm, and they can be manufactured from synthetic, semi-synthetic, and natural components through physicochemical routes, such as solvent evaporation, spray-drying, and anionic polymerization methods, respectively [ 118 , 119 , 120 ]. As represented in Figure 5 C, microparticles are convenient as they can be manipulated to formulate solid, semi-solid, and liquid products that can be administered orally, intravenously, intramuscularly, or subcutaneously to successfully deliver and enhance the efficacy and bioavailability of one or more drugs [ 121 ].…”