Investigating the Effect of Different Grades and Concentrations of Ph‑sensitive Polymer on Preparation and Characterization of Lidocaine Hydrochloride as in Situ Gel Buccal Spray

Abstract

Objective: The present study was aimed to develop a pH-triggered in situ gel for local release of lidocaine hydrochloride (lidocaine HCL) in the buccal cavity to improve the anesthetic effect of this amino amide drug which has very high water solubility. The formulations were introduced to the oral cavity as a spray to improve compliance and for easier administration.Methods: In this work, two grades of carbopol (934 and 940)-based in situ gel spray were designed. The formulations containing lidocaine HCl 5% were prepared by mixing different concentrations of carbopol with xanthan gum. Eight formulations were investigated and evaluated for gelation capacity, spray angle, volume of solution delivered per each actuation, rheological properties, and release kinetic model. Similarity factor (f2) was used for the comparison of dissolution profiles.Results: The prepared formulations undergo gelation after it had been actuated to the buccal cavity as a spray solution. The results showed that, as the concentration of polymer was increased, the release of drug decreased and the viscosity increased for both grades. The spray angle and volume of solution delivered per each actuation varied according to the composition of each formulation. The in situ gel containing 0.3% carbopol 934 and 0.2% xanthan gum regarded as a better candidate which had a good gelation and release property compared to other formulations. Drug release from optimized in situ gel spray followed Korsmeyer–Peppas model and was mediated by Fickian diffusion mechanism.Conclusion: Lidocaine HCl-loaded pH-sensitive in situ gel was successfully developed using carbopol 934 as polymer to be applied to the buccal cavity as spray solution for more effective anesthetic effect and painless treatment.

Perspective Impact of Gelling Agents on the Mechanistic Behavior for the Topical Delivery of Flufenamic Acid Nano-Ethosomal Dispersion

“…This is because the polymer concentration increased the degree of cross-linking, which caused more water molecules to be trapped and held in the carbopol structure, which resulted in a vicious and rigid structure. 28,29 Similar results were observed with Quercus infectoria extract herbosomal gel. 30 Furthermore, formulas containing carbopol 940 (G3 and G4) are more viscous than formulas containing carbopol 934 (G1 and G2) with the same polymer concentration.…”

Frovatriptan succinate intranasal delivery for brain targeting – in vivo study.‎

“…There are several migraine treatment formulations, but the limitations of drug delivery systems have hampered development (16). While intranasal (IN) drug delivery is an attractive option, its main disadvantages are small nasal cavity capacity (0.2 mL), anterior leakage, and mucociliary clearance, which might impair the effectiveness of the nasal medication delivery system (17,18). Migraine is defined by intense pain and increased sensitivity to sensory stimuli, leading to a decrease in regular daily activities.…”

“…In situ gelling systems that are ion-activated include gellan gum and sodium alginate, whereas temperaturedependent methods include Pluronics, Tetronics, and polymethacrylates (e.g., Carbopol and cellulose acetate phthalate) (18,43,44). In situ, gels provide several advantages over typical gels, such as being simpler to produce, injectable as a liquid, and able to remain on the surface of the nasal cavity for a longer time owing to gelling (45)(46)(47)(48)(49)(50).…”

Formulation and Characterization of Intranasal Drug Delivery of Frovatriptan-Loaded Binary Ethosomes Gel for Brain Targeting

“…The main disadvantages are small nasal cavity capacity (0.2 mL), anterior leakage, and mucociliary clearance, which might impair the effectiveness of the nasal medication delivery system. [24][25][26][27][28] In situ, gels provide several advantages over typical gels, such as being simpler to produce, injectable as a liquid, and able to remain on the nasal cavity's surface for a longer time owing to gelling and mucoadhesion. 29,30 The current study aims to prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosomes.…”