INTRODUCTION:

Acne vulgaris or simply known as acne is a human skin disease characterized by skin with scaly red skin (seborrhea), blackheads and whiteheads (comedones), pinheads (papules), large papules (nodules), pimples and scarring. Acne affects skin having dense sebaceous follicles in areas including face, chest and back. Acne may be of inflammatory or non-inflammatory forms. Due to changes in pilosebaceous unit’s lesions are caused by androgen stimulation. Acne occurs commonly during adolescence, affecting about 80–90% of teenagers in the Western world and lower rate are reported in rural societies.

Acne is usually caused by increase in androgens level like testosterone mainly during puberty in both male and female. Acne reduces over time and tends to disappear over the age. The large nodules called as cysts and severe inflammatory acne called as nodulocystic. The cystic acne occurs on buttocks, groin, armpit area, hair follicles and perspiration ducts and affects deeper skin tissue than common acne. Acne causes scarring and psychological effects such as; reduced self-esteem and in rare cases depression or suicide. Reports showed the incidence of suicidal tendency in patients with acne as about 7.1%. Acne usually occurs during adolescence. The word acne refers to the presence of papules, scars, comedones and pustules. The common form of acne is known as acne vulgaris. Many teenagers suffer from this type of acne. Acne vulgaris shows the presence of comedones. Acne rosacea is synonym for rosacea and some persons not have acne comedones associated with their rosacea, hence prefer the term rosacea. Chloracne occurs due to exposure to polyhalogenated compounds.¹Tinospora cordifolia commonly named as “Guduchi” in Sanskrit belonging to family Menispermaceae is a genetically diverse, large, deciduous climbing shrub with greenish yellow typical flowers, found at higher altitude. In racemes or racemose panicles, the male flowers are clustered and female are solitary. The flowering season expands over summers and winters. A variety of active components derived from the plant like alkaloids, steroids, diterpenoid lactones, aliphatics, and glycosides have been isolated from the different parts of the plant body, including root, stem, and whole plant. Recently, the plant is of great interest to researchers across the globe because of its reported medicinal properties like anti-diabetic, anti-periodic, anti-spasmodic, anti-inflammatory, anti-arthritic, anti-oxidant, anti-allergic, anti-stress, anti-leprotic, anti-malarial, hepatoprotective, immunomodulatory and anti-neoplastic activities.³

MATERIALS AND METHODS:

Materials:

The main ingredient used in our formulation is Tinospora cordifolia which is commonly known as gurjo, guduchi or giloy etc. It belongs to the family Menispermaceae. Potential medicinal properties reported by scientific research include anti-microbial, anti-diabetic, antipyretic, antispasmodic, anti-inflammatory, anti-arthritic, antioxidant, anti-allergic, anti-stress, anti-leprotic, antimalarial, hepato-protective, immuno-modulatory and anti-neoplastic activities.³

Excipients that are used in our formulation are as follows:

Paraffin wax (hard):- Hard paraffin is a mixture of solid hydrocarbons, also known as paraffin wax. It is used to stiffen ointments and creams.⁴

a) Wool fat: Wool fat is a pale yellow, tenacious substance with a faint but characteristic odour. It is insoluble in water and a high proportion of water may be incorporated with it by melting (m.p. 36–42°C) and stirring. Wool fat is used as an emollient base for creams and ointments.⁵

b) Triethanolamine: Triethanolamine is also said to help in the emulsification of various ingredients, which is one of the primary reasons it is used in creams and other product formulations.

Emulsification is the process of mixing two immiscible liquids, mostly an oil and non-oil liquid, to form a more homogenous product.⁶

c) White soft paraffin: White Soft Paraffin is a soft unctuous mass and is poorly soluble in water and alcohols but is soluble in methylene chloride. As such it is a useful product to use in liquids, creams, emulsions and ointments, of which, ointments will only be considered within this body of work. WSP is an excellent carrier material (base) for active dermatological ingredients as well as acting as a barrier to the environment, providing moisturising trapping, oily characteristics preventing evaporation of water to the environment.⁷

d) Liquid Paraffin: Liquid paraffin is a mixture of liquid hydrocarbons. It is used as skin moisturizer in ointments.⁸

e) Glycerine: Glycerin functions as a denaturant, fragrance ingredient, hair conditioning agent, humectant, oral care agent, oral health-care drug, skin protectant, skin conditioning agent—humectant, and viscosity-decreasing agent.⁹

f) Xanthan gum: Xanthan gum exhibits great compatibility with thickeners present in the market such as cellulose derivatives, starch, pectin, gelatin, dextrin, alginate, and carrageenan. By combining various gums with xanthan gum in altered proportions. It performs better after modiﬁcation with enzymatic treatments which results in the removal of galactose residues.¹⁰

g) Methyl paraben: Methyl paraben is a methyl ester of p-hydroxybenzoic acid. It is a stable, non-volatile compound used as an antimicrobial preservative in foods, drugs and cosmetics for over 50 years.¹¹

h) Perfume (Rose water): Rose water ointment, or cold cream, was used as a soothing, producing fragrance, cooling application for superficial lesions of the skin.¹²

i) Extract of Tinospora cordifolia.

Methods:

The cream is of o/w type. It is prepared by using the fusion method.

Preparation of the o/w emulsion cream: The oil-soluble and the emulsifiers are mixed in a container in a water bath. In a separate beaker of water, preservatives and water-soluble components are added. After the oil phase has been heated, it is placed in a mortar and pestle, and the water phase is gradually added and triturated until a clicking sound can be examined. At the end, preservatives and a few additives are added.¹³

a) Formulation of Cream Base.

The oil phase was prepared by melting the waxes at 75^∘C and mixing the ingredients uniformly. The aqueous phase was prepared by dissolving the water-soluble ingredients in deionized water. The water phase was warmed to 75–80^∘C until all ingredients were dissolved. When the water and oil phase were at the same temperature, the aqueous phase was slowly added to the oil phase with moderate agitation and was kept stirred until the temperature dropped to 40^∘C. The emulsion was cooled to room temperature to form a semisolid cream base.

Methyl Paraben was dissolved in warmed deionized water, and the solutions were added to the cream base using an overhead stirrer. The mixture was stirred for 15 min until the formulation became uniform.¹⁴

Fig.1 Cream base.

b) Formulation of extract.

Fresh T. cordifolia stem was chopped into small pieces, and the content of moisture was estimated by heating a weighted portion of the biomass at 105 °C until constant weight. The rest of the biomass was shade dried until the moisture content was reduced to < 2% of the initial moisture content. The dried biomass was ground to fine powder form using agate mortar and pestle, and it was sieved using sieve having a mesh size of 300 μm and the larger fractions were discarded. Extraction of phenolics from the dried biomass was performed in a capped conical flask using methanol with varying amount of de-ionised water as the extraction solvent for approximately 72hours. Extraction experiments were also optimised in terms of temperature and time. The solvent to the solute ratio of 5:1 (v/w) and stirring rate of 800 rpm were maintained for all the extraction experiments.

The conical flask was fitted with a reflux condenser for all the experiments performed at a temperature > 20 °C. After the stipulated period the contents of the conical flask were subjected to sonication on ultrasonic cleaning bath (Cole-Parmer LK08895-06) at 40 kHz for 20 min for enhanced recovery of plant phenolics. After ultrasound-assisted extraction, filtration was performed to recover the solid biomass.¹⁵

The filtration was then evaporated upto 5% extract is remained using heating mantle.

Fig.2 Maceration

Fig.3 Filtration

Fig.4 Evaporation

FORMULATION TABLE:

Variable concerntration of Tinospora cordifolia was taken and F5 was found to be optimized. The formula was set according to the standards.

Table 1. Formulation table

Sr. No	Ingredients	F1	F2	F3	F4	F5
1.	Extract (Tinospora Cordifolia)	5%	10%	15%	20%	25%
2.	Paraffin hard	0.5 gm	0.5 gm	0.5 gm	0.5 gm	0.5 gm
3.	Wool fat	1 gm	1 gm	1 gm	1 gm	1 gm
4.	White soft paraffin	5 gm	5 gm	5 gm	5 gm	5 gm
5.	Liquid paraffin	1 ml	1 ml	1 ml	1 ml	1 ml
6.	Glycerin	1 ml	1 ml	1 ml	1 ml	1 ml
7.	Xanthan Gum	0.5 gm	0.5 gm	0.5 gm	0.5 gm	0.5 gm

4. EVALUATION PARAMETERS:

a) Determination of pH: The pH of the cream can be measured on a standard digital pH meter at room emperature by taking adequate amount of the formulation diluted with a suitable solvent in a suitable beaker.

b) Physical appearance: The physical appearance of the cream can be observed by its colour, roughness and graded.

c) Spreadability: Adequate amount of sample is taken between two glass slides and a weight of 100gm is applied on the slides for 5 minutes. Spreadability can be expressed as,

S= m*l/t

Where,

m = weight applied to upper slide.

l = length moved on the glass slide.

t = time taken.

d) Viscosity: Viscosity of formulated creams can be determined by using Brookfield Viscometer.

e) Homogeneity: The formulation was tested for the homogeneity by visual appearance and by touch.

f) Dye test: The scarlet dye is mixed with the cream. Place a drop of cream in a slide and cover with a cover slip and examine it under a microscope. If the disperse globule appears red and the ground colourless then it is o/w type and the reverse condition appears in w/o type of creams.

g) After feel: Emolliency, slipperiness and amount of residue left after the application of fixed amount of cream was checked.

h) Type of smear: After application of cream, the type of film or smear formed on the skin were checked.

i) Irritancy study: Mark an area of 1sq.cm on the left-hand dorsal surface. The cream was applied to the specified area and time was noted. Irritancy, erythema, edema was checked, if any, for regular intervals upto 24hrs and reported.¹⁶

Fig.5. Final Preparation.

RESULTS:

The anti-acne cream was found to be safe and not cause any irritation. All the evaluation parameters performed like pH determination, Physical appearance, Spreadability, Viscosity, Homogeneity, Removal, Dye test, After feel, Type of smear, Irritancy study, etc are under expected limits.

The Antimicrobial activity shown by our formulation is proved by following picture.

Fig.6. Antimicrobial activity of Tinospora cordifolia.

The results for evalution parameters are as follows:

Table 2. Evaluation parameters and results

Sr.No	Evaluation Parameters.	Results.
1.	Determination of pH	5.0-6.5
2.	Physical appearance	a) Colour- slightly brownish b) Roughness- no roughness found etc.
3.	Spreadability	Was easily spreaded Spreadabilty value= 0.53.
4.	Viscosity	0.10 Pa·s to 15 Pa·s
5.	Homogeneity	Was found to be smooth
6.	Dye test	It was observed as o/w type of emulsion.
7.	Irritancy study	No irritancy was found

CONCLUSION:

As the world is shifting towards natural products our product is herbal one and the preparation shows antimicrobial activity for reducing the acnes which has been proved at laboratory level. We have prepared 5 formulations F1, F2, F3, F4, F5, among which F5 was found to be optimized. Various evalution parameters are performed and are found under expected limits.

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Received on 02.02.2024 Modified on 11.03.2024

Res. J. Pharmacology and Pharmacodynamics. 2024;16(2):85-89.

DOI: 10.52711/2321-5836.2024.00015