Development and optimization of ciprofloxacin-loaded gelatin microparticles by single-step spray-drying technique

Abstract

Polymeric particles are a versatile class of local or systemic drug delivery systems, used to improve drugs pharmacokinetics and pharmacodynamics along with patient compliance. Herein, we report a rapid, scalable, and optimized method to encapsulate ciprofloxacin (CP x ), a poor water soluble antimicrobial agent, in gelatin microparticles by single step processing via spray-drying of an aqueous solution. The developed particles show mainly a wrinkle morphology with a unimodal distribution, with mean diameters ranging between 2 and 4 μm, depending on the processing conditions. The encapsulation of 1, 2 and 5 wt% CPx narrows the size distribution (1-3 μm). In vitro release experiments showed that up to 80% of encapsulated drug is released during the first 6 h, and the release kinetics was best fitted with the Korsmeyer-Peppas model, explained by the superimposition of drug diffusion and polymer chain relaxation. The minimal inhibitory concentrations against S. aureus and E. coli, obtained from pure and encapsulated ciprofloxacin, demonstrated that the spray-drying process does not inhibit the drug's bioactivity or the process feasibility. Thus, spray-drying of protein-drug particle systems is an advantageous method to produce microparticles with potential to lung delivery systems. Smith, M. L. & Sencadas, V. (2018). Development and optimization of ciprofloxacin-loaded gelatin microparticles by single-step spray-drying technique. Powder Technology, 330 201-209. Abstract:Polymeric particles are a versatile class of local or systemic drug delivery systems, used to improve drugs pharmacokinetics and pharmacodynamics along with patient compliance. Herein, we report a rapid, scalable, and optimized method to encapsulate ciprofloxacin (CPx), a poor water soluble antimicrobial agent, in gelatin microparticles by single step processing via spray-drying of an aqueous solution. The developed particles show mainly a wrinkle morphology with a unimodal distribution, with mean diameters ranging between 2 and 4 , depending on the processing conditions. The encapsulation of 1, 2 and 5 wt% CPx narrows the size distribution (1-3 m). In vitro release experiments showed that up to 80% of encapsulated drug is released during the first 6 hours, and the release kinetics was best fitted with the Korsmeyer-Peppas model, explained by the superimposition of drug diffusion and polymer chain relaxation. The minimal inhibitory concentrations against S. aureus and E. coli, obtained from pure and encapsulated ciprofloxacin, demonstrated that the spraydrying process does not inhibit the drug`s bioactivity or the process feasibility. Thus, spray-drying of protein-drug particle systems is an advantageous method to produce microparticles with potential to lung delivery systems.

Application of biodegradable microsphere injections: an anticancer perspective

“…The preparation methods of gelatin microspheres include emulsification method, 36 condensation method 37 and spray drying method. 38 Gelatin microspheres can be used for tumor embolization therapy, 39 which can be injected into the designated blood vessels to block the nutrient supply of the tumor.…”

Micro and nanoscale technologies in oral drug delivery

“… [ 137 ] Ciprofloxacin Ciprofloxacin, a water-insoluble antimicrobial drug, was encapsulated in gelatin as a result of a one-step process by spray drying an aqueous solution. [ 138 ] Polymethacrylic acid-polyethylene glycol-chitosan Insulin Surface thiolation was used to increase the drug release performance of hydrogel-based oral insulin delivery systems. [ 139 ] Chitosan-carboxymethyl starch 5-aminosalicylic acid Chitosan-carboxymethyl starch particles were synthesized via a casting technique with high encapsulation performance as a drug delivery system for the colon.…”

Cosmetic, Biomedical and Pharmaceutical Applications of Fish Gelatin/Hydrolysates

“…The loading efficiency was over 94% and the drug was released within the first 6 h. It was proven that ciprofloxacin had anti- staphylococcus aureus and E. coli activity and showed minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) values equivalent to pure ciprofloxacin. The spray-drying of the protein-drug particle system was an advantageous alternative to emulsions—it provided higher productivity and had a potential for pulmonary delivery of drugs [ 94 ].…”