Design of antihistaminic transdermal films based on alginate–chitosan polyelectrolyte complexes: characterization and permeation studies

Abstract

The purpose of this study was to develop suitable matrix-type transdermal drug delivery systems of Ketotifen fumarate (KF) as antiasthmatic drugs. Chitosan-alginate polyelectrolyte complex (PEC) films were used as drug release regulators for KF. Antihistaminic films with variable PEC compositions were prepared using different ratios of chitosan (CTS) to sodium alginate (ALG). Propylene glycol (PG) was used as plasticizer; Tween 80 (T) and Span 20 (S) were used as permeability enhancers. Nine formulations were obtained by film casting method and characterized in terms of weight uniformity, thickness, folding endurance, moisture lost, and moisture absorption. In addition, drug release and permeation through rat abdominal skin mounted in Franz cell were investigated. All formulations were found to be suitable in terms of physicochemical characteristics, and there was no significant interaction between the used drug and polymers. It was noticed that when T is used as permeation enhancer, a satisfactory drug release pattern was found where 99.88% of drug was released and an amount of 2.121 mg/cm of KF was permeated after 24 h. For the optimal formulation, a permeability coefficient of 14.00 ± 0.001 cm h and a latency time of 0.35 ± 0.02 h were found. The in-vitro analysis showed controlled release profile which was fitted by Korsmeyer-Peppas model (R = 0.998). The obtained results suggested that new controlled release transdermal formulations of asthmatic drugs could be suitably designed as an alternative to the common forms.

Biocompatible non-covalent complexes of chitosan and different polymers: Characteristics and application in drug delivery

“…The effect of insulin released from microparticles was conserved during more than 60 h, implying its long-term stability in vivo. Lefnaoui et al (16) developed chitosan/alginate PEC-based matrix-type films for transdermal delivery of ketotifen fumarate (Tab. I).…”

“…More recently, numerous PECs based on polysaccharides and proteins have been formulated as carriers for drug delivery, DNA delivery, or tissue engineering (2,4,7). Many different polyanions have been used for the formation of PECs with chitosan, such as natural polymers and their semi-synthetic derivatives (e.g., alginates (13)(14)(15)(16)(17)(18), pectin (19)(20)(21)(22)(23), xanthan gum (11,12,(24)(25)(26)(27), carrageenan (28)(29)(30), carboxymethylcellulose (31,32), collagen (25)), synthetic polymers and tripolyphosphate (TPP) (33) (Tab. I).…”

Preparation of Hybrid Alginate-Chitosan Aerogel as Potential Carriers for Pulmonary Drug Delivery

“…The characteristics of the resultant hybrid polyelectrolyte depend on many factors such as polymer concentration, charge density, molecular weight, ionic strength, pH of the mixture, reaction temperature, and mixing ratio and procedure [ 34 , 35 ]. Recently, increasing applications are proposed for alginate/chitosan polyelectrolyte including food engineering [ 36 , 37 ], a free-standing membrane for drug delivery, wound dressing application [ 38 , 39 ], and drug delivery [ 40 ].…”

Preparation of Metronidazole Containing Film Dosage Forms from Sodium Alginate

“…Alg-Na has been widely used as a food additive, a tablet disintegrator, or a gelling agent [9,10]. A thin film can be simply prepared with Alg-Na using the casting method without the need for dissolution in organic solvents or heating [11][12][13]. Film Dosage forms (FDs) are films that contain therapeutically active compounds.…”