INTRODUCTION:

Lignocaine is used as a local anaesthetic and it is a first amino amide local anaesthetic.¹ It is also known as lidocaine. This medication is used to numb tissue in a specific area. It is also used to treat ventricular tachycardia and to perform nerve block. Lignocaine gel is applied directly to the skin or mucous membrane. Lignocaine is soluble in water, Ethanol, benzene ethyl ether, and chloroform. IUPAC name of Lignocaine is 2-(diethylamino)-N-(2, 6-dimethylphenyl) acetamide hydrate hydrochloride. Lignocaine settles the neuronal layer by restraining the ionic motions required for the commencement and conduction of driving forces, in this manner affecting neighborhood sedative action^1-2.

Lidocaine is a nearby sedative of the amide type. It is utilized to give nearby sedation by nerve bar at different destinations in the body.

It does as such by balancing out the neuronal layer by restraining the ionic motions required for the inception and conduction of driving forces, in this way affecting nearby sedative activity. Specifically, the lidocaine specialist follows up on sodium particle channels situated on the interior surface of nerve cell layers. At these channels, impartial uncharged lidocaine atoms diffuse through neural sheaths into the axoplasm where they are along these lines ionized by getting together with hydrogen particles. The resultant lidocaine cations are then able to do reversibly restricting the sodium channels from within, keeping them secured an open express that forestalls nerve depolarization. Therefore, with adequate blockage, the layer of the postsynaptic neuron will at last not depolarize and will in this way neglect to transmit an activity potential. This encourages a sedative impact by not only forestalling torment signals from engendering to the cerebrum however by prematurely ending their age in any case^3-4.

Notwithstanding blocking conduction in nerve axons in the fringe sensory system, lidocaine effectively affects the focal sensory system and cardiovascular framework. After ingestion, lidocaine may cause incitement of the CNS followed by sorrow and in the cardiovascular framework, it acts basically on the myocardium where it might create diminishes - in electrical volatility, conduction rate, and power of contraction⁵.

MATERIALS AND METHODS:

Material:

Lignocaine hydrochloride (Ozone international, Mumbai), Carbopol 934, propylene glycol, methyl paraben, propyl paraben distilled water and triethanolamine were taken from laboratory grade.

Equipment:

Weighing balance (Shimadzu AY220), Brookfield Viscometer (Brookfield LV-DV-E viscometer), pH meter (Equiptronics pH meter Model No. EQ-615), UV Visible Double beam spectrophotometer (Systronic 2201).

Methods:

Preparation of Gel:

· Accurately weighed Carbopol 934 was taken in a beaker and dispersed in 50ml distilled water.

· Kept the beaker aside to swell the Carbopol for half an hour and then stirring was done.

· 5ml of propylene glycol was taken in another beaker and added weighed quantity of propyl paraben and methyl paraben and stirred properly.

· After all, Carbopol was dispersed, 2gm of lignocaine hydrochloride and preservatives solutions were added with constant stirring.

· Finally, Distilled water was added to make up the volume up to 100ml and triethanolamine was added drop wise in the formulation⁵.

Table 1. Formulation Table

Sr. no.	Ingredients	Quantity Taken			Role
Sr. no.	Ingredients	F1	F2	F3	Role
1	Lignocaine Hydrochloride	2gm	2gm	2gm	API
2	Carbopol 934	0.5gm	1gm	1.5gm	Gelling agent
3	Propylene Glycol	5ml	5ml	5ml	Humectant
4	Methyl paraben	0.1gm	0.1gm	0.1gm	Preservative
5	Propyl Paraben	0.1gm	0.1gm	0.1gm	Preservative
6	Triethanolamine	0.6ml	0.6ml	0.6ml	Thickening agent
7	Distilled Water	q.s.	q.s.	q.s.	Solvent

Evaluation of Lignocaine Hydrochloride Gel^6-7:

Percentage Yield:

To determine the percentage yield the empty container was weighed first and then gel formulations were added and it is again weighed. Then by subtracting the empty container weighed with the container containing gel formulation gives the practical yield.

Drug Content:

To determine the drug content the 10gm of gel formulations were transferred in 250ml of volumetric flask containing 20ml of alcohol and it was stirred for 30 minutes. The volume was made upto 100ml and filtered. 1ml of above solution was further diluted using alcohol upto 10ml and again 1ml of the above solution was taken and further diluted upto 10ml with alcohol. The absorbance was measured at 252nm using Uv-visible Spectroscopy.

Determination of pH:

The pH of gel formulations were determined by using digital PH meter. 1gm of gel was dissolved in 100ml of distilled water and stored for 2 hours. The Measurement of PH was determined.

Spreadability:

To determine the Spreadability the gel formulation of 1gm was placed between the horizontal plates (20×20 cm²) after 1 minute. The upper plate was tied with a standardized weight of 125gm.

Extrudability:

To determine the Extrudability of gel formulation the collapsible metal or aluminium collapsible tube was filled with gel formulation and the pressure was applied to the tube so that extrusion of gel takes place and it was checked.

Viscosity:

Selection of spindle:

Spindle T₆₄ used for the determination of Viscosity of Lignocaine Hydrochloride Gel.

Sample Container size:

The viscosity was measured using 100gm of gel filled in a 100ml beaker.

Spindle immersion:

The T₆₄ was lowered perpendicular in the center taking care that spindle does not touch the bottom of the beaker.

Measurement of viscosity:

The T₆₄ was used for the determination of viscosity in gels. The factors like temperature, pressure, and Sample size etc which affects the viscosity was maintained during the process. To give various Viscosities the helipath T bar spindle was moved up and down. The Torque reading was found to be 22%. The viscosity of gel was obtained by taking average of 3 reading in 1minutes.

In vitro- Diffusion Study:

The diffusion studies were carried using Franz diffusion cells. The donor compartment containing 1gm of gel was separated from receptor compartment containing 26ml of PBS pH 6.8 by a treated cellophane membrane. The receptor compartment was agitated throughout the process by magnetic stirrer. The samples were withdrawn at scheduled intervals (replaced with equivalent amount of PBS pH 6.8) and analysed at 217.6 nm in double beam UV-Visible spectrophotometer.

RESULT AND DISCUSSION:

Table 2: Percentage yield of gel formulations

Formulation	Percentage yield
F1	98.11%
F2	99.54%
F3	97.44

Table 3: Drug Content of gel formulations

Formulation	Drug Content
F1	95.78
F2	98.47
F3	96.75

Table4. pH of gel Formulations

Formulation	pH
F1	4.48
F2	5.68
F3	7.42

Table 5: Viscosity of gel formulations

Formulation	Viscosity (cP)
F1	5432
F2	2220
F3	6345

Table 6: Spreadability of gel Formulations

Formulation	Spreadability(gm.cm/s)
F1	8.43
F2	11.54
F3	13.43

Table 7: Extrudability of gel formulations

Formulation	Extrudability
F1	+
F2	+++
F3	++

Excellent (+++), Good (++), Average (+), Poor (-)

Figure 1: In-vitro Diffusion Studies of F1, F2 and F3 Batches

Table 8: Invitro Diffusion Study

Time	%CDR
	F1	F2	F3
0	0	0	0
30	48.88	14.41	29.18
60	57.06	25.92	42.93
120	66.25	43.40	47.67
180	74.34	62.17	71.09
240	92.56	80.29	83.17
300	95.35	96.30	93.06

CONCLUSION:

Carbopol 934 was used as a polymer in various batches. Developed Formulations of Physicochemical parameters such as percentage yield, drug content, pH, Viscosity, Spreadability and Extrudability were carried out for developed batches of Lignocaine Hydrochloride. In-vitro Diffusion studies were carried out, F2 batch shows better results than that of the other two batches i.e. 96.06%. Viscosity studies of various formulations Exhibited that Formulation F2 was better than that of F1 and F3. From among all the developed formulation, F2 Shows better rheological properties and excellent Extrudability. pH of the F2 Batch is Sufficient to treat the pain. Percentage yield and drug content of F2 batch is good than other batches. F2 Batch is suitable for topical use than other batches. So F2 Batch shows the good results than other Batches.

ACKNOWLEDGMENT:

Authors are thankful to Principal, College of Pharmacy.

AUTHORS CONTRIBUTION:

All Authors Contributed equally.

CONFLICT OF INTEREST:

Nil.

REFERENCES:

1. Pandit A, Pol V, Kulkarni V. Xyloglucan Based In-Situ Gel of Lidocaine HCl for the Treatment of Periodontosis. Journal of Pharmaceutics 2016;1(1):1-9.

2. https://en.wikipedia.org/wiki/Lidocaine.

3. Tektook N, Ali A. Lidocaine Hydrochloride (Local). The American Society of Health-System Pharmacists 2015;2(1):123-129.

4. Hasan F, Ali A. (Lidocaine Hydrochloride (Antiarrhythmic). The American Society of Health-System Pharmacists 2015;12(3):156-165.

5. Mitkari B, Korde S, Mahadik K. Formulation and evaluation of topical liposomal gel for fluconazole. Indian Journal of Pharmaceutical Education 2014;44(4):324-333.

6. Kasar P, Phadtare D, Kale K. Formulation ad evaluation of Antifungal gel containing Itraconazole. International Journal of Current Pharmaceutical Research 2018;10(4):71-74.

7. Basha B, Prakasam K, Goli D. Formulation and evaluation of gel containing fluconazole antifungal agent. International Journal of Drug Development and Research 2011;3(4):109-128.

Received on 13.04.2020 Modified on 24.05.2020

Research J. Pharm. and Tech. 2021; 14(2):908-910.

DOI: 10.5958/0974-360X.2021.00161.X