In vitroCiprofloxacin release from poly(lactide-co-glycolide) microspheres

Abstract

Biodegradable microspheres of PLGA (75:25 and 50:50) containing Ciprofloxacin (CIPRO) were prepared by two different procedures based on: (i) solvent-evaporation, and (ii) evaporation-extraction of the organic phase. The encapsulation rates from the different formulations were quite variable, as well the release patterns of the drug from the microspheres. The evaporation-extraction method seems to be more efficient for the CIPRO encapsulation compared with the solvent evaporation method. The 50:50 PLGA composition released the drug faster and showed degradation signs after incubation in aqueous medium in both manufacturing methodologies.

Bioinspired superamphiphobic surfaces as a tool for polymer- and solvent-independent preparation of drug-loaded spherical particles

“…7). This initial rapid release can be attributed to the drug particles localized at the surface, which can rapidly dissolve in the aqueous medium, as previously observed for other hydrophilic drugs encapsulated in nano-and microspheres of PLGA [35,36,38]. It should be noted that ciprofloxacin hydrochloride has a high solubility in water (3.5 g/ 100 ml) and drug crystals rapidly dissolve in the release medium [31]; therefore drug crystals encapsulated in the most external region of PLGA particles can complete the dissolution in few hours.…”

“…In the present work, subsequent hardening of the droplets on the superamphiphobic surfaces ensured 100% ciprofloxacin encapsulation yield, as the contact of the drug with the surface is minimum during the particle processing. It should be noticed that the highest loading tested corresponded to 0.2 mg drug mg À1 of microparticle, which is one order of magnitude greater than those previously attained by encapsulating ciprofloxacin in PLGA particles via solvent-evaporation and evaporation-extraction methods [35]. Compared to other active substances and methods to prepare spherical particles, such as the precision particle fabrication (PPF) technology [36], the superamphiphobic-surface-based method is advantageous in terms of total amount of drug encapsulated (nearly 10 times greater), encapsulation efficiency (100% vs. 50-90%), and simplicity in terms of liquid phases used and processing set-up and time.…”

“…The release was more sustained as the solvent found it difficult to enter into the hydrophobic matrix. The hydrolysis of PLGA chains requires some time to cause changes in the spherical particles structure that may lead to an erosion-accelerated release of the remaining encapsulated drug [35,38]. Triphasic drug release profiles have been previously reported for PLGA microparticulates and implants; namely an initial burst phase, followed by a slow continuous release step or a lag phase and finally a second rapid release phase [39].…”

Preparation and Characterization of Eudragit Rs 100 Microspheres Containing Ciprofloxacin Hydrochloride

“…HCl-Eudragit RS 100 microspheres were prepared via emulsion solvent evaporation method. Martinez et al (1997) have reported the preparation of poly (DL-lactide-coglycolide,PLGA) ciprofloxacin microspheres. They used both the solvent evaporation method and the evaporation-extraction method to prepare sustained release biodegradable microspheres.…”

Synthesis of ciprofloxacin-conjugated poly (L-lactic acid) polymer for nanofiber fabrication and antibacterial evaluation

“…28 The release of ciprofloxacin from a polymer matrix (implant of screw and microsphere) has been attempted. [29][30][31][32] The ester carbonyl of aliphatic polyester may also help in binding to hard M III -cations, in addition to carbonyl oxygen donors in amides, and ultimately inhibit bacterial proliferation. Drug conjugated nanofibers can also mitigate scarring and pain in patients because of their hydrolytic quality and the subsequent enzymatic degradation of PLA into carbon dioxide and water.…”