• 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.


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


1. Peppas NA, Langer R. New challenges in biomaterials. Science 1994;263:1715-20.
2. Suisha F, Kawasaki N, Miyazaki S, Shirakawa M, Yamatoya K, Sasaki M, et al. Xyloglucan gels as sustained release vehicles for the intraperitoneal administration of mitomycin C. Int J Pharm 1998;172:27-32.
3. Miyazaki S, Endo K, Kawasaki N, Kubo W, Watanabe H, Attwood D, et al. Oral sustained delivery of paracetamol from in situ gelling xyloglucan formulations. Drug Dev Ind Pharm 2003;29:113-9.
4. Tushar N, Nayan G, Bhushan R, Sunil B, Pawar SP. In situ gel: Novel approach in sustained and controlled drug delivery system. Int J Pharm Sci 2013;4:1-18.
5. Jones MR, Philip B. Massersmith BP. In-situ forming biomaterials, oral maxillofacial surgery. Clin North Am 2002;14:29-38.
6. Qiu Y, Park K. Environment-sensitive hydrogels for drug delivery. Adv Drug Deliv Rev 2001;53:321-39.
7. Soppimath KS, Aminabhavi TM, Dave AM, Kumbar SG, Rudzinski WE. Stimulus-responsive: “Smart” hydrogels as novel drug delivery systems. Drug Dev Ind Pharm 2002;28:957-74.
8. Sonawan M, Shinkar D, Saudagar R. Mucoadhesive buccal drug delivery system: Review article. Int J Curr Pharm Res 2017;9:1-4.
9. Thosar MM. Intra oral sprays-an overview. Int J Pharm Life Sci 2011;2:1235-46.
10. Lee HS. Recent advanced in topical anesthesia. J Dent Anesth Pain Med 2016;16:237-44.
11. Meechan JG. Effective topical anesthetic agent and techniques. Dent Clin N Am 2002;46:759-66.
12. Estafan DJ. Invasive and noninvasive dental analgesia techniques. Gen Dent 1998;46:600-3.
13. Ogle OE, Mahjoubi G. Local anesthesia: Agents, techniques, and complications. Dent Clin North Am 2012;56:133-48, 9.
14. Hu L, Silva SM, Damaj BB, Martin R, Michniak-Kohn BB. Transdermal and transbuccal drug delivery systems: Enhancement using iontophoretic and chemical approaches. Int J Pharm 2011;421:53 62.
15. Ghosh S, Roy G, Mukherjee B. Dental mold: A novel formulation to treat common dental disorders. AAPS Pharm Sci Tech 2009;10:692 702.
16. Pagar SA, Shinkar DM, Saudagar RB, Development and evaluation of in situ nasal mucoadhesive gel of metoprolol succinate by using 32full factorial design. Int J Pharm Pharm Sci 2014;6:218-23.
17. Pandit AP, Pol VV, Kulkarni VS. Xyloglucan based in situ gel of lidocaine HCl for the treatment of periodontists. J Pharm 2016;2016:1 9.
18. Moffat AC, Osselton MD, Widdop B, Galichet LY. Clarke’s Analysis of Drugs and Poisons. 4th ed. London: Pharmaceutical Press; 2011. p. 1573.
19. Harish NM, Prabhu P, Charyulu RN, Gulzar MA, Subrahmanyam EV. Formulation and evaluation of in situ gels containing clotrimazole for oral candidiasis. Indian J Pharm Sci 2009;71:421-7.
20. Joshi M, Bolmal U, Dandagi P. Formulation and evaluation of cefuroxime axetil sol gel for periodontits. Int J Pharm Pharm Sci 2014;6:498-503.
21. Guhel MC, Nagori SA. Fabrication of modified transport fluconazole transdermal spray containing ethyl cellulose and Eudragit® RS100 as film formers. AAPS Pharm Sci Tech 2009;10:684-91.
22. Gupta C, Juyal V, Nagaich U. Formulation and optimization of a thermosensetive in situ gel of moxifloxacine hydrochloride for ocular drug delivery. Int J App Pharm 2018;10:123-30.
23. Murtaza G. Development of glutaraldehyde cross-linked metronidazole loaded chitosan microcapsules: Analysis of dissolution data using DD-Solver. Latin Am J Pharm 2011;30:301-8.
24. Shahzad MK, Ubaid M, Raza M, Murtaza G. The formulation of flurbiprofen loaded microspheres using hydroxyl propyl methyl cellulose and ethyl cellulose. Adv Clin Exp Med 2013;22:177-83.
25. Costa P, Sousalobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001;13:123-33.
26. Patil S, Kadam A, Bandgar S, Patil S. Formulation and evaluation of an in situ gel for ocular drug delivery of anticonjunctival drug. Cellul Chem Tech 2015;49:35-40.
27. Troy DV, Hauber MJ, Brien MA. Remington, the Science and Practice of Pharmacy. 21st ed. Philadelphia, PA, USA: Lippincott Williams and Wilkins; 2006. p. 771.
28. Katzbauer B. Properties and applications of xanthan gum. Polym Degrad Stab 1998;59:81-4.
29. Deshpande JM, Shah PB. Formulation and development pH induced in-situ gelling system of an anti-infective drug for sustained ocular drug delivery. J Pharm Sci Biosci Res 2012;2:238-44.
30. Nandgude T, Thube R, Jaiswal N, Deshmukh P, Chapta V, Hire N. Formulation and evaluation of pH induced in situ gel of salbutamol sulphate. Int J Pharm Sci Nanotech 2008;1:177-83.
31. Phaechamud T, Charoenteeraboon J, Saengthongpinit W, Chuekaew A. Spray pattern of oral cavity sprays containing the herbal extracts. Res J Pharm Bio Chem Sci 2012;3:1301-6.
32. Bisht NN, Goswami L, Kothiyal P. Preparation and evaluation of in situ topical oral gel of levofloxacine by using combination of polymer. Ind J Drug 2014;2:142-51.
33. Aslani A, Ghannadi A, Najafi H. Design, formulation and evaluation of a mucoadhesive gel from Quercus brantii L. And Coriandrum sativum L. As periodontal drug delivery. Adv Biomed Res 2013;2:21.
34. Kumara P, Prakash SC, Lokesh P, Manral KK. Viscoelastic properties and rheological characterization of carbomer. Int J Latest Res Eng Tech 2015;1:17-30.
35. Das S, Samantha A, Bose A. Design, development and evaluation of fluconazole topical gel. Asian J Pharm Clin Res 2015;8:132-5.
36. Kumar AS, Gupta VN, Guda DV, Sivadasu P. Formulation and development of in situ forming gel for the treatment of oral thrush. Asian J Pharm Clin Res 2018;11:342-6.
37. Kipo SL, Oppong EE, Kwakye KO. Physicochemical evaluation and tablet formulation properties of shea tree gum. Asian J Pharm Sci 2014;7:121-7.
38. Salih OS, Nief RA. Effect of natural and synthetic polymer on the properties of candesartan cillexetil matrix tablet prepared by dry granulation. Asian J Pharm Clin Res 2016;9:161-70.
39. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems -review. Acta Poloniae Pharm Drug Res 2010;67:217-23.
40. Nagarwal RC, Srinatha A, Pandit JK. In situ forming formulation: Development, evaluation, and optimization using 33 factorial design. AAPS Pharm Sci Tech 2009;10:977-84.
171 Views | 216 Downloads
How to Cite
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.
Original Article(s)