Mucoadhesive Dosage form of Lidocaine Hydrochloride: I. Mucoadhesive and Physicochemical Characterization

Abstract

The aim of this study was to characterize a buccal mucoadhesive film using lidocaine and its hydrochloride salt (LDHCL) as a model drug. Buccal films were developed using carbopol 971P as a mucoadhesive polymer, and glycerol as a plasticizer. Scanning Electron Microscope, Differential Scanning Calorimetry, X-ray powder diffraction, and Fourier Transform Infra Red techniques were used to characterize the mucoadhesive films. Bioadhesive properties were evaluated using the Universal Instron Instrument with chicken pouch as a model tissue. LDHCL and its base were present in carbopol 971P films in a molecular dispersion state without exerting any effect on the glass transition of these films. The mucoadhesive force between the chicken pouches and the film containing glycerol did not change by time during the tested period (1-20 min), while increased with increasing the amount of glycerol (10-40% w/w of polymer content). Furthermore, a linear increase in the mucoadhesive force was accompanied by the increase in the film thickness, while a linear decrease followed by plateau was obtained when loading the patch with LDHCL at concentration above 1 mg/cm(2). Loading carbopol film with lidocaine base, in a concentration up to 6 mg/cm(2) decreased linearly the mucoadhesive properties, which could be attributed to salt formation between the acidic carboxylic moiety of carbopol and basic lidocaine.

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

“…1g, lidocaine HCl powder showed a N-H stretching at 3383 cm-1, a C-H stretching at 3011 cm-1, an amide I (C=O) at 1654 cm-1 and an amide II (C-N) at 1472 cm-1. These values are in good agreement with the results obtained in other studies [29,37,38]. Regardless of the PVP content, the ATR-FTIR spectrum of lidocaine HCl matrices showed no absence of any functional peak in the spectra, revealing that there is no significant chemical interaction between the drug and polymers.…”

“…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.…”

“…These results assured that lidocaine HCl was dispersed with the polymer network as a molecular dispersion level. Previous studies showed that lidocaine HCl was present in the amorphous condition in a hydroxypropyl cellulose film [27] and carbopol film [29]. …”

Dental Mold: A Novel Formulation to Treat Common Dental Disorders

“…3a) and lidocaine hydrochloride (Fig. 3b) shows that all the characteristic peaks of amoxicillin trihydrate and lidocaine hydrochloride are present (34,35). Again, the FTIR spectra of the combination of both drugs (Fig.…”

Studying the Effect of Different Variables on the Formulation of Mucoadhesive Buccal Patches of Captopril

“…There was a significant increase (P<0.05) in mucoadhesive and bond strength as PG concentration increased because the addition of plasticizer agents reduced the internal stress of the patch by decreasing the glass transition temperature of the polymer and thus increasing mucoadhesion forces [27].…”