Development of bioadhesive chitosan gels for topical delivery of lidocaine

Abstract

Lidocaine (LC) is a local anesthetic agent. The aim of this study is prolonging the anesthetic effect of this drug for transdermal delivery. Gels of LC hydrochloride were prepared with three different molecular weights (MW) and concentrations of chitosan. lecithin was used as permeation enhancer. Viscosity, bioadhesion, drug release from synthetic membranes, drug permeation through the biological barrier (rat skin) and antinocicetive effect of gels were studied. Increasing the concentration of chitosan caused to decrease the bioadhesion. Drug release studies in gels showed that increasing the concentration and MW of chitosan caused an increase in both the rate and extent and also in flux of drug probably because of the increase in repulsive forces between LC and chitosan cations. The flux of drug through the rat skin was higher for 3% high MW chitosan gel (H3) compared to the standard gel. LC was effective topically in hind paw formalin assay. It was most active immediately after its administration. The analgesic activity of LC in H3 gel could cover the duration of the formalin nociception. The maximal response of LC in comparable doses of H3 and standard gel was about 52% and 36% analgesia in the second phase, respectively compared to the control group.The higher response of the H3 gel may be attributed to the bioadhesive effect of chitosan base and the higher concentrations of LC compared to the standard gel.

Lyophilized Sustained Release Mucoadhesive Chitosan Sponges for Buccal Buspirone Hydrochloride Delivery: Formulation and In Vitro Evaluation

“…In a previous study, Foda et al (26) reported that the release of tramadol HCl from L-CH sponges was slower than from H-CH sponges because smaller pore sizes were evident in L-CH sponges compared to sponges prepared by higher grades of chitosan. In another study, Varshosaz et al (39) stated that the release of lidocaine from uncross-linked chitosan films increased as the molecular weight of chitosan increased. Lidocaine release from L-CH films was slower than that from M-CH films, and the highest release was obtained from H-CH films.…”

Potential of recovered proteins from invasive green crabs (Carcinus maenas) as a functional food ingredient

“…Although their size causes a challenge in utilizing them as a human food, the shell and minced meat of green crabs have potential for utilization by the food industry. The crustacean exoskeleton contains chitin, which has a wide range of applications in industries such as food and agriculture, cosmetics, nutraceuticals, pharmaceuticals and textiles . Many applications for crab shell derivatives have been reported in the scientific literature, whereas there are a limited number of studies on minced crab meat and its potential application in food products.…”

Preparation and Characterization of Poly (Vinyl Alcohol)–poly (Vinyl Pyrrolidone) Mucoadhesive Buccal Patches for Delivery of Lidocaine HCL

“…There are several pharmaceutical dosage forms of lidocaine HCl available on the market, i.e., solution for injection or infusion, nasal spray, oral gel and transdermal patch [24,26]. Several authors have developed the buccal mucoadhesive systems of lidocaine and/or lidocaine HCl [25,[27][28][29]. However, in previous literature, no attempt has been taken to formulate lidocaine HCl buccal patches simply using PVA and PVP along with Eudragit S100.…”