PREPARATION AND EVALUATION OF CIPROFLOXACIN/CHITOSAN IMPLANTS AS A CONTROLLED BIODEGRADABLE DRUG DELIVERY SYSTEM

This work aimed to prepare and evaluate physically crosslinked
implantable matrices based on chitosan as a site-specific
delivery of ciprofloxacin hydrochloride (CFX.HCl) for the
prevention of post-surgical wound infection. Biodegradable
matrices were prepared from chitosan and different polyanion
polymers by direct compression. The potential of formulation
variables on the in-vitro drug release from polymeric matrices has
been studied. A matrix system of CFX.HCl based on the polyanion
complex of chitosan and pectin showed a sustainable drug release
over three days. The swelling and in-vitro drug release experiments
suggested that complex formation between chitosan and pectin has
occurred at ratio 1:2. The results also suggested that CFX.HCl
release from chitosan matrices was markedly influenced by the
nature of polyanion polymers, mixing ratio and total weight of
matrices, whereas the compression force did not significantly affect
the drug release. With increasing CFX.HCl loading, a decrease of
the percent cumulative release was observed. Approximately 13%
of loaded drug was released from matrix containing 25% w/w drug
during 72 hrs in phosphate buffer pH 7.4. Fitting the in-vitro drug
release data to Korsmeyer equation indicated that combined effect
of diffusion and polymer chain relaxation could be the mechanisms
of drug release. Microbiological simulated test revealed the
efficient microbial inhibitory effect of chitosan: pectin (1:2) matrix
with 25% drug load over extended period of time.
In conclusion: Cross-linked chitosan implantable device for
septic wounds or post surgical treatment with antimicrobial
capability and wound healing properties was developed to serve as
a site-specific delivery system for antibiotics.