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

  • Halah Talal Sulaiman Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
  • Saba Abdulhadi Jabir Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
  • Khalid Kadhem Al-kinani Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.

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.

Keywords: Lidocaine Hydrochloride, Carbopol, In situ gel.

Author Biographies

Halah Talal Sulaiman, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
Departament of pharmaceutics
Saba Abdulhadi Jabir, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
Department of pharmaceutics
Khalid Kadhem Al-kinani, Department of Pharmaceutics, College of Pharmacy, University of Baghdad, Baghdad, Iraq.
Department of phrmaceutics

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Sulaiman, H. T., S. A. Jabir, and K. Kadhem Al-kinani. “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”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 11, no. 11, Nov. 2018, pp. 401-7, doi:10.22159/ajpcr.2018.v11i11.28492.
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