Abstract
Chitosan (CHI) and chitosan/poly(2-ethyl-2-oxazoline) (CHI/POZ)-based films were prepared by casting from aqueous solutions of polymer blends with different compositions. Ciprofloxacin was used as a model drug in these formulations. The weight, thickness, folding endurance and transparency of blend films were measured and characterised. All films had a uniform thickness (0.06 ± 0.01 mm) and exhibited sufficient flexibility. The surface pHs of films ranged from 3.76 ± 0.49 to 4.14 ± 0.32, which is within the pH range suitable for vaginal applications. The cumulative release of the drug from the films in experiments in vitro was found to be 42 ± 2% and 56 ± 1% for pure CHI and CHI/POZ (40:60) films, respectively. Drug-free chitosan/poly(2-ethyl-2-oxazoline) films showed weak antimicrobial activity against Escherichia coli. Drug-loaded CHI and CHI/POZ films showed good antimicrobial properties against both Gram-positive Staphylococcus aureus and Gram-negative bacteria Escherichia coli. Mucoadhesive properties of these films with respect to freshly excised sheep vaginal mucosa were evaluated using a tensile method. It was established that all films were mucoadhesive, but an increase in POZ content in the blend resulted in a gradual reduction of their ability to stick to vaginal mucosa. These films could potentially find applications in vaginal drug delivery.
Highlights
Vaginal drug administration has traditionally been used for the delivery of contraceptive agents and hormones as well as for local therapy of infections [1]
We report the preparation of chitosan/poly(2-ethyl-2-oxazoline) films loaded with ciprofloxacin as a model drug
Polymeric films based on chitosan (CHI) and its blends with poly(2-ethyl-2-oxazoline) (POZ) were cast by the solvent evaporation method according to a protocol previously reported by our group with minor modifications [29]. 1% w/v aqueous solutions of CHI and POZ were prepared by dissolving pre-weighed amount of dry polymers at room temperature
Summary
Vaginal drug administration has traditionally been used for the delivery of contraceptive agents and hormones as well as for local therapy of infections [1]. The dosage forms traditionally used for vaginal drug delivery include creams, gels, pessaries, tablets, and elastomeric rings [2,3,4,5]. Mucoadhesive polymeric films have received interest as a potential formulation strategy for vaginal delivery of contraceptives, microbicides and antimicrobial agents [6]. All water-soluble polymers have some ability to adhere to mucosal tissues, i.e., they exhibit mucoadhesive properties [7,8]. Charged polymers of higher molecular weight show greater ability to adhere to mucosal membranes compared to non-ionic and smaller macromolecules
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