Formulation and Evaluation of Chewable Lozenges Containing Guava Leaves Extract and Clove Oil for Dental Caries

Dental Caries: People of all ages can get dental caries, often known as tooth decay, which is very frequent in Thailand (66–90% in 2007). Streptococcus mutans, a bacteria that grows in biofilms on tooth surfaces and generates acid from fermentable carbohydrates like sucrose, is the primary culprit. Caries and demineralization result from this acid's dissolution of tooth minerals. Fillings, root canals, and antibacterial treatments are available forms of treatment; nevertheless, prevention through good dental hygiene (brushing, mouthwash, and flossing) is essential. Oral care solutions contain chemicals like triclosan and chlorhexidine; however, excessive usage of these chemicals can result in negative side effects like inflammation and tooth discoloration. Therefore, as a possible  substitute  for  caries,  herbal  products  with  anti-cariogenic  qualities  are being investigated.[5]

Fig.1.1 Tooth Decay

Sugary foods are broken down by oral bacteria, which results in the production of acids, primarily lactic acid. These acids cause the enamel on our teeth to lose minerals and soften by lowering the pH of the plaque. [9] If the acids persist, they may penetrate deeper tooth layers and cause more harm. However, the minerals calcium, phosphate, and fluoride can aid in the surface healing of the enamel when the pH in the mouth returns to normal as a result of saliva. A white spot on the tooth, which can still be repaired with the right care, forms if the pH remains low for an extended period of time. Sleeping and eating are two everyday activities that can be severely impacted by toothaches. The World Health Organization states that since dental problems, such as caries, impact up to 90% of school-age children and people globally and may impede development and well-being, minimizing tooth discomfort should be a top focus in global oral health activities. [1]

Tooth pain, or toothache, is caused by irritation of the nerve in the tooth's root or surrounding tissues and can be either sudden and acute or chronic and persistent. It is often due to dental issues such as infections, decay, trauma, or tooth loss, and may also result from tooth extractions. In some cases, pain may feel like it originates in the teeth but is actually referred from areas like the ear, sinuses, or TMJ. Toothaches can significantly impact daily activities like eating and sleeping. According to the World Health Organization, reducing tooth pain should be a priority in global oral health initiatives, as dental issues, including caries, affect up to 90% of school-age children and adults worldwide, potentially hindering development and well-being. [1]

Fig.1.1 tooth decay Causes of dental carries

Toothache can be caused by either dental or non-dental (non-odontogenic) conditions.

Dental

1. 1. Hypersensitivity of the dentin
   2. Periodontal
   3. Impaction of food
   4. Abscess of the periodontals
   5. Ulcerative gingivitis with acute necrotizing [ANUG]

Non-dental

1. 1. 1. Myofascial pain
      2. Psychogenic toothache
      3. Acute and chronic sinusitis
      4. Angina pectoris [classical, refer to muscle pain]
      5. Trigeminal zoster
      6. Trigeminal neuralgia

Symptoms

1. Pain in your jaw or teeth while eating.
2. Headaches and sensitivity to cold or hot foods.
3. Bleeding or pus coming from the gums or around atooth.
4. Swelling in your jaw or around atooth.
5. Injury or trauma to the area.
6. Bad Breath.

Diagnosis

A dentist or endodontist will first collect a patient's medical history, inspect the painful area, and perform tests in order to diagnose a toothache. They might tap the tooth to feel for decay, redness, or swelling. To see the tooth's response, cold therapy is another option. Other potential reasons, such as disorders with the temporomandibular joint (TMJ), sinus infections, or ear troubles, should be ruled out. To determine the precise source of the discomfort, X-rays may be obtained.

Lozenges

A lozenges is a solid drug that has both local and systemic effects and dissolves gradually in the mouth [11]. Lozenges, which get their name from the French term for a diamond, are used to relieve pain and treat oral diseases by calming the mouth or allowing medicine to enter through the lining of the mouth. They are particularly beneficial for people who have trouble swallowing pills and for progressive drug release. Since the 20th century, pharmacists have produced lozenges, such as pastilles and troches. [1] Herbal lozenges can be used as pain relievers or antiseptics, as well as to relieve congestion and soothe the throat. They function by releasing active chemicals that are uniformly distributed throughout the mouth or throat's afflicted region. The lozenges are simple to use and come in precise dosages for efficient relief of throat irritation. [17]

Types of lozenges

1. Hard candy lozenges

sugar syrups are used to make hard candy lozenges. These are mixtures of sugar, other carbohydrates, and herbal excipient that are amorphous or glassy. [9]

2. Soft candy lozenges:

Soft lozenges are becoming more and more popular due to their adaptability and ease of making on-the-spot for a variety of drugs. The bases are often composed of a variety of polyethylene glycols, acacia, or similar substances. One variety of these soft lozenges is the pastille, which is defined as a soft, transparent lozenge that contains an a drug in a foundation of gelatin, glycerogelatin, or acacia: sucrose.

3. Chewable Lozenges:

They often taste slightly acidic and have a strong flavor. It's not too hard to cook them. They are an excellent way to administer medication because fruit-flavored products may often sufficiently mask the drug's taste. [13]

Fig.1.2 lozenges

2. Review Of Literature

1. Anjali V. Telgote , Prachi P. Udapurkar et al(2024) A common and frequently incapacitating ailment, toothaches can have a major negative influence on a person's quality of life. For this reason, it is crucial to establish a convenient and efficient alleviation strategy. The creation and assessment of medicated lozenges intended especially to relieve toothaches is the main focus of this study. Lozenges are a simple, non-invasive method of managing pain that has a localized effect. Choosing suitable active pharmaceutical ingredients (APIs) with established analgesic and anti-inflammatory qualities, including clove oil, was part of the formulation process. [9]

2. Suvarna T et al(2024) Chewing gum is a portable way to give medication. It can be used locally or systemically to administer drugs orally. Significant advancements in technology and research pertaining to the oral medicine administration route have been made in recent years. Throughout the year, medicated chewing gum has drawn interest from all around the world because of its capacity to increase patient compliance in both young and old patients as well as the general public.

3. Apeksha Sadashiv Ghuge and Khandre RA et al(2024) guava, or Psidium guajava Linn., is utilized as a food and a traditional medicine in subtropical regions worldwide due to its pharmacologic properties. It has been established that this plant's pharmacological properties include anti-inflammatory, anti-nociceptive, anti-hepatoprotective, anti-allergy, antibacterial, antispasmodic, cardioactive, and antidiabetic effects.

4. Ali Ali1, Wissam Zam 2 and Walaa Ibrahim et al(2022) ) Lozenges are oral medications in a variety of shapes that often contain both a medical ingredient and a flavoring. These days, they are widely used to deliver various active ingredients in pharmaceutical and food preparations. Since the medicinal substances are well absorbed through the buccal lining or when eaten, they are designed to lessen both local and systemic symptoms. Lozenges offer a number of benefits, including ease of administration to both young and old patients and ease of preparation requiring little time or equipment. [13]

5. Pooja Mishra, Jitendra Banweer, Praveen Tahilani, Prem Samundre and sarika shrivastava et al(2022) In order to cure mouth ulcers, the purpose of this study was to create and assess a herbal chewing gum that contained extracts of powdered Psidium guajava leaves and Curcuma longa Linn rhizomes. Guava leaves have traditionally been used to treat a number of illnesses, including cough, sore throat, diabetes mellitus, diarrhea, and wounds. They also have a calming effect. Turmeric has antibacterial, anti-inflammatory, and virucidal properties, while guava has tannins, triterpenes, pentacyclic triterpenoid, guajanoic acid, saponins, carotenoids, ellagic acid, amritoside, betasitosterol, uvaol, oleanolic acid, andursolicacid.

6. Akbal ahmad,abadhesh kumar niranjan et al(2021) After being cleaned with running tap water to remove any debris, the freshly picked guava leaves were left to dry at room temperature in the shade for three to four weeks. The dried guava leaves were ground into a coarse powder using a mechanical grinder and then run through sieve number 40. In a conical flask, 100 g of powdered dried guava leaves were macerated in 250 ml of ethanol, chloroform, and water for 24 hours at room temperature with periodic shaking. A straight forward filtration technique was used to remove the mixture after 24 hours, and the filtrates weregatheredin different vessels. [28]

7. Rupali chanda, lavanya nallaguntla et al(2020) to create and assess lozenges for a sore throat that contained loratadine. The oral route is the most popular of the numerous administration routes due to a number of factors, including ease of consumption, adaptability, and especially patient compliance.

8. Nalita Phaiboon, Pawitra Pulbutr, Bunleu Sungthong, Sakulrat Rattanakiat et al(2019) Dental caries is mostly caused by Streptococcus mutans. The purpose of this study was to examine how the cariogenic qualities of Streptococcus mutans were affected by the ethanolic extracts of Psidium guajava, Glycyrrhiza glabra, and Syzygium aromaticum. These therapeutic plants have long been utilized as the components of herbal mouthwashes to treat tooth cavities..

9. Chandrawanshi Mayuri J., Sakhare R. S., Dr. Nagoba Shivappa N. and Bhalekar Rohini V.Channabasweshwar et al(2018) Lozenges are a firm, pleasant dose form that is administered orally. These are medicinal dose forms with flavors that are intended to be sucked and held in the mouth or pharynx. They typically contain one or more medications in a sweetened foundation. Lozenges have a local action in the oral cavity at a specific location. Additionally, a lozenge has a systemic effect, meaning that the medication circulates in the bloodstream and demonstrates its pharmacological action. [1]

11. Devkar Mohan J 1, Shaikh Shahrukh S. M.1, Amol G. Jadhao3, Miss. Jayshri Sanap4, Prashant A. Patil5 et al(2013) Coughing is one of the most prevalent issues that everyone encounters. There are two different kinds of cough: dry cough and wet cough. There is cough secretion or mucus in a wet cough, but there is neither in a dry cough. Due to its ease of patient compliance, the syrup is the most often used and well-liked dose form for treating colds and coughs. The primary ingredients of the herbal cough syrup were honey, pudina, tulsi, or cinnamon, which were primitive medications.

3. Rationale Of the Study: -

Need Of Work: -

? Dental caries is a common oral health problem, and prevention is key. Herbal lozenges that combine these ingredients can help prevent decay by reducing bacteria in the mouth, improving gum health, and promoting remineralization of tooth enamel.

? Guava leaves and clove oil are well-known for their antimicrobial, anti-inflammatory, and pain- relieving properties, which can help prevent and manage dental caries (tooth decay) naturally.

? With growing concerns about the side effects of synthetic chemicals in oral care products, herbal formulations like guava and clove-based lozenges provide an alternative that may be perceived as safer and more gentle, particularly for people with sensitivities or those seeking more holistic health options.

? Lozenges are easy to use, portable, and convenient. For individuals who are looking for quick and effective relief or prevention, lozenges offer an easy-to-consume form that delivers the benefits of these herbal ingredients.

Objectives: -

1. To study the guava leaves, clove oil and their beneficial properties.
2. To study the antimicrobial properties of guava leaves and clove oil.
3. To study medicinal uses of formulation.
4. To study the effect formulation against dental caries .
5. To maintain the good oral health.

4. Plan Of Work: -

• Selection of crude drug

1. Guava leaves

2. Clove

3. Pippermint Oil

• Collection Of Crude Drug

• Preparation of material and methods

1. Selection of the effective method of preparation.

• Experimental design-

• Formulation and preparation of lozenge

• Result & discussion

• Conclusion

• Reference

5. Selection Of Crude Drug

1. Guava leaves

Botanical Name: Psidium gaujava Linn.

Synonyms:

• Psidium pomiferum Linn.
• Psidium pyriferum Linn.
• Family: myrtaceae

Category: antioxidants, flavonoids, essential oil

Chemical constituent

Guava leaves is composed of volatile oil ,flavonoids ,alkaloids.it contain many phenolic compound ,including quercetin ,kaempferol ,apigenin catechin chlorogenic acid ,hyperin , gallic acid ,also contain essential oil including ,linalool, eucalyptol ,limonene ,

Uses

1. • Treatment of diarrhea, dysentery, and gastroenteritis.
   • Management of diabetes.
   • Relief from fever and cough.
   • Treatment of skin conditions like acne and wounds.
   • Oral health: gum inflammation and toothache relief.
2. Clove oil:

Botanical Name: Syzygium aromaticum (Linn) Merr. & L.M.Perry

Synonyms:

1. Eugenia caryophyllata Thunb.

2. Eugenia aromatica (Linn) Baill.

Family: Myrtaceae

Property : antioxidant ,anti-inflammation

Chemical constituent

1. 1. Volatile oils (90-95%):
      • Eugenol (70-85%)
      • Beta-caryophyllene (5-10%)
      • Humulene (2-5%)
      • Limonene (1-2%)
   2. Phenolic compounds:
   3. Flavonoids:

Uses

1. Dental care: toothache, gum inflammation, and mouthwash.
2. Digestive issues: nausea, diarrhea, and bloating.
3. Respiratory problems: cough, cold, and bronchitis.
4. Skin and mucous membrane: wounds, acne, and insect bites.

3. Pippermint

Botanical Name: Mentha Piperita Linn.

Synonyms:

1. Mentha viridis Linn.

2. Mentha × piperita Linn.

Family: Lamiaceae (Mint family)

Property: antimicrobial, antioxidant, analgesic

Chemical constituent

1. Volatile oils

Menthol (35-45%)

Menthone (20-30%)

Methyl acetate (5-10%)

2. Flavonoids
3. Phenolic acids

Uses :

• Digestive issues: indigestion, nausea, irritable bowel syndrome (IBS).
• Respiratory problems: cough, cold, bronchitis, asthma.
• Skin and mucous membrane: itching, inflammation, acne.
• Oral health: mouthwash, gum inflammation, bad breath.

6. MATERIAL AND METHODS

Guava leaves, clove oil, peppermint, sucrose, corn starch gelatine ,water

2. Glassware’s And Instruments:

Beaker, Stirrer, Weighing balance, Container ,Spatula ,hot plate

Collection of Drug:

The Guava leaves powder was collected from Ayurgyan and Clove oil was collected From RV essential. The Authentification of drug done by following method Physical Analysis:

1.Guava leaves powder:

1.Color: Green

2.Odor: Characteristic

3.Taste: Slightly bitter

2. Clove oil :

Thin layer chromatography (TLC):

This is an analytical tool that can be used to identify eugenol and other chemical component In clove oil.

METHOD:

Formulation of guava leaves extract: To make the plant extract, fresh guava leaves were cleaned to get rid of any debris and then allowed to dry for three to four weeks in the shade. The leaves were filtered after being dried and pulverized into a coarse powder. In separate flasks, 100g of the powdered leaves were soaked in 250 ml of ethanol, chloroform, and water for a full day, with periodic shaking, in order to extract the leaves. The mixture was filtered after a day in order to separate the liquid extract from the solid components. In order to acquire the plant extract, the solvent was finally extracted from the liquid using a rotary vacuum evaporator set to 45 to 50°C [11].

Formulation of lozenges:

Lozenges were made by dissolving sucrose in water to produce a syrup, which was then heated until it thickened. The drug and additional ingredients were added after 30 minutes and blended in while the heating process went on. [13] After that, the material was put into molds and let to cool for ten to fifteen minutes. The lozenges were taken out of the molds once they had solidified. [5]

Preparation of lozenges

1. 1. Guava leaves extraction

Fig.6.3 lozenges

1. Appearance

Look            Visual inspection was done on the prepared chewable lozenges to check for color, clarity, and the presence of any suspected particles.

2. Stickiness and grittiness

By gently rubbing the prepared chewable lozenge sample between two fingers, the product's texture—specifically, its stickiness and grittiness—was assessed visually.

3. pH

Using a digital pH meter calibrated by standard solutions at pH 4-7, the pH of each chewable lozenge was ascertained. The pH was measured after one gram of the weighed formulation was dissolved in 100 milliliters of distilled water.

4. Thickness

Using a vernier caliper, thickness was measured and reported in millimeters.

5. Diameter

The moulds used determine the diameter, size, and form of the lozenges. Although lozenges can be created in a variety of sizes and shapes, they are typically round with flat or biconvex faces.

6. Stability Studies

The stability study was conducted , the Chewable lozenges were tightly packed and stored at a cooling temperature (4°C) for three months, and the changes in the properties(appearance, stickiness and grittiness, pH, thickness and dissolution) was evaluated.

7. In-vitro Antibacterial Activity

Antibacterial Activity in Vitro Staphylococcus aureus, Escherichia coli, and Streptococcus mutans isolated colonies were subjected to in vitro antimicrobial tests. The zone of inhibition and the minimum inhibitory concentration (MIC) were determined using the Agar well diffusion method. Agar plates that had been prepared for testing were used to cultivate the bacterial strains.

Observation table:

We conduct several tests and procedures in the results, and the values obtained are recorded in this observation table. This observation table contains the pH, thickness, diameter, and other organoleptic property values.