Films based on chitosan polyelectrolyte complexes for skin drug delivery: Development and characterization

Abstract

a b s t r a c tNovel chitosan based polyelectrolyte complexes (PEC) were developed and optimized in order to obtain films possessing the optimal functional properties (flexibility, resistance, water vapour transmission rate and bioadhesion) to be applied on skin. The development was based on the combination of chitosan and two polyacrylic acid (PAA) polymers with different crosslinkers and crosslinking densities. The interaction between the polymers was maximized controlling the pH, and by forming the films at a pH value close to the pK a of the respective components as identified by potentiometric and turbidimetric titrations. The action of glycerol, PEG200, Hydrovance and trehalose upon the functional properties of the films was also evaluated. Glycerol was found to improve the film properties in terms of flexibility, resistance and water vapour transmission rate (WVTR) with a maximum effect at 30%. The application of a pressure sensitive adhesive (PSA) significantly improved bioadhesion with a negligible influence in the resistance and flexibility of the films.The optimized film, including adhesive, has shown very good properties for application in the skin and represents a very promising formulation for further incorporation of drugs for topical and transdermal administration.

Biopolymer-Based Transdermal Films of Donepezil as an Alternative Delivery Approach in Alzheimer’s Disease Treatment

“…It expresses the capability of a material to resist changes of shape without crack formation. Films intended for transdermal drug delivery must be flexible enough to follow the movements of the skin (18,22). It has been reported that an ideal transdermal film should be soft and tough that can be characterized by a high elongation value (23,24).…”

“…Elongation at break (%) indicates the flexibility of films and it has been defined as the ratio between the extension of the film at the point of rupture and the initial length of the sample (18). Elongation testing of sodium alginate-based transdermal films of DNP (TF-CONT, TF-LM1, TF-LM3, and TF-LM5) was performed using texture profile analyzer (TA-XT Plus, Stable Micro Systems, Surrey, UK) equipped with a 5-kg load cell.…”

Preparation and In Vitro Evaluation of Chitosan Nanoparticles Containing Diclofenac Using the Ion-Gelation Method

“…The endothermic peak in CS thermogram might be related to the glass transition temperature (Tg) of Cs and the exothermic peak at 325°C was probably due to degradation of the polymer (22)(23)(24). Thermograms of nanoparticle formulations were the same and showed only a broad endothermic peak around 140 -170°C.…”

Design, Characterization, and In Vitro Evaluation of Antifungal Polymeric Films

“…CB solutions (1% w/v) were prepared by dissolving in water. The pH of the solutions was adjusted at 1 by addition of 1 M HCl, in order to avoid precipitation when mixing the solutions of the polymers (13,29). Both CH and CB solutions were filtered through Miracloth® (Calbiochem-Novabiochem Corp., San Diego, CA) to remove impurities prior to use.…”

“…Specifically, films based on CH have been mainly developed for food packaging (9), or for pharmaceutical applications. In the latter case, different administration routes and uses such as buccal delivery of flufenamic (10), control release of amoxicillin in stomach for the treatment of Helicobacter pylori (11), vaginal delivery of metronidazole for the treatment of bacterial vaginosis (12), or potential skin drug delivery systems (13) were evaluated. Several works have studied the mechanical properties of CH films, demonstrating that these properties may be improved when CH forms polyelectrolyte complexes with other polymers oppositely charged (14,15).…”