Formulation And Evalution of Herbal Mucoadhesive Buccal Patch

FORMULATION TABLE –

MECHANISM OF ACTION OF CORIANDER IN MOUTH ULCER-

The essential oil from the coriander plant has also been used traditionally in the Asian region to stimulate gastric secretion and treat gastric ulcers, and mouth infections[3].

Anti-Inflammatory Effects

1.         Inhibition of pro-inflammatory cytokines: Coriander's active compounds, such as linalool and beta-pinene, may inhibit the production of pro-inflammatory cytokines, reducing inflammation and pain in the oral mucosa.

2.         Antioxidant activity: Coriander's antioxidants may neutralize free radicals, reducing oxidative stress and inflammation in the oral mucosa.

Antimicrobial Effects

1.         Inhibition of microbial growth: Coriander's essential oils, such as linalool and beta-pinene, may inhibit the growth of microorganisms, reducing the risk of infection and promoting healing.

2.         Disruption of microbial membranes: Coriander's essential oils may disrupt the membranes of microorganisms, ultimately leading to their death.

Analgesic and Anesthetic Effects

1.         Activation of TRPV3 receptors: Coriander's active compounds, such as linalool, may activate TRPV3 receptors, which can help reduce pain and inflammation.

2.         Inhibition of pain mediators: Coriander's active compounds may inhibit the production of pain mediators, such as prostaglandins and bradykinin, reducing pain and discomfort.

Mucoadhesive Properties

1.         Interaction with mucin: Coriander's active compounds may interact with mucin, a key component of the oral mucosa, enhancing the mucoadhesive properties of the buccal patch.

2.         Prolonged release of active compounds: The mucoadhesive properties of coriander may facilitate the prolonged release of its active compounds, providing sustained therapeutic effects.

 By incorporating coriander into a buccal patch, these mechanisms of action may help alleviate symptoms.

MECHANISM OF ACTION OF TURMERIC IN MOUTH ULCER-

Turmeric, a spice commonly found in Indian and Middle Eastern cooking, has been used for centuries in traditional medicine to treat various health issues, including mouth ulcers. Here's a breakdown of the mechanism of action of turmeric in mouth ulcers[4]:

Anti-Inflammatory Effects

1.         Inhibition of pro-inflammatory enzymes: Turmeric's active compound, curcumin, inhibits the production of pro-inflammatory enzymes, such as cyclooxygenase-2 (COX-2) and lipoxygenase (LOX).

2.         Reduction of inflammatory cytokines: Curcumin reduces the production of inflammatory cytokines, such as tumor necrosis factor-alpha (TNF-alpha) and interleukin-1 beta (IL-1β).

Antioxidant Effects

1.         Neutralization of free radicals: Curcumin neutralizes free radicals, which can damage oral mucosa cells and contribute to mouth ulcer formation.

2.         Enhancement of antioxidant enzymes: Curcumin enhances the activity of antioxidant enzymes, such as superoxide dismutase (SOD) and glutathione peroxidase (GPx).

Antimicrobial Effects

1.         Inhibition of microbial growth: Curcumin inhibits the growth of microorganisms, such as bacteria and fungi, which can contribute to mouth ulcer formation.

2.         Disruption of microbial membranes: Curcumin disrupts the membranes of microorganisms, ultimately leading to their death.

Wound Healing Effects

1.         Enhancement of collagen synthesis: Curcumin enhances the synthesis of collagen, an essential protein for wound healing.

2.         Improvement of tissue regeneration: Curcumin improves tissue regeneration by promoting the proliferation and differentiation of oral mucosa cells. Associated with mouth ulcers, such as pain, inflammation, and infection.

Analgesic and Anesthetic Effects

1.         Inhibition of pain mediators: Curcumin inhibits the production of pain mediators, such as prostaglandins and bradykinin.

2.         Activation of opioid receptors: Curcumin activates opioid receptors, which can help reduce pain perception.

Its inflammatory effects are expressed in the reduction in the inflammatory cytokines IL-6 and IL-8. Furthermore, the reduction in fibrotic cicatricial function is expressed by inhibiting fibroblasts and myoblasts (type I and III collagen) of the oral mucosa.

MUCOADHESIVE BUCCAL DRUG DELIVERY SYSTEM-

Oral route is the most preferred route for the delivery of any drug. Drug delivery via the membranes of the oral cavity can be subdivided as[5-6]:-

•           Sublingual delivery: This is systemic delivery of drugs through the mucosal membranes lining the floor of the mouth.

•      Buccal delivery: This is drug administration through the mucosal membranes lining the cheeks (buccal mucosa).

•      Local delivery: This is drug delivery into the oral cavity.

Within the oral mucosal cavity, the buccal region offers an attractive route of administration for controlled systemic drug delivery. Buccal delivery is the administration of drugs through the mucosal membrane lining the cheeks. Although the sublingual mucosa is known to be more permeable than the buccal mucosa, the latter is the preferred route for systemic transmucosal drug delivery. This is because the buccal mucosa has an expanse of smooth muscle and relatively immobile mucosa, which makes it a more desirable region for retentive systems. Thus, the buccal mucosa is more appropriate for sustained direction of drug delivery.

Herbs Used In Buccal Patch :

•           Coriander :

Synonyms :    Fructus coriandri, Coriander fruits, Cilantro, Chinese parsley.

Biological Source :    Coriander consists of

dried ripe fruits of Coriandrum sativum Linn., belonging to family Umbelliferae.

Chemical Constituents : Coriander consist of about 1% of volatile oil the chief volatile components are D-(+)-linalool (coriandrol), along with other constituents like, borneol, p- cymene, camphor, geraniol, limonene, and alpha-pinenes. The fruits also contain fatty oil and hydroxycoumarins. The fatty oils include acids of petroselic acid, oleic acid, linolenic acid, whereas the hydroxycoumarins include the umbelliferone and scopoletine [7].

Uses :

1.         Antimicrobial and Antifungal Properties :

Coriander's antimicrobial and antifungal properties, when used in buccal patches, can prevent and treat oral infections, maintaining oral hygiene, particularly beneficial for patients with gingivitis, thrush, or mouth ulcers.[8]

2.         Anti-inflammatory Effects :

Coriander's flavonoids and terpenes are anti-inflammatory compounds, aiding in the reduction of oral inflammation, making it a promising treatment for oral mucositis and other related issues.

3.         Antioxidant Benefits :

Coriander, rich in antioxidants, protects oral tissues from oxidative stress, potentially preventing oral cancer and periodontal disease, and can be incorporated into buccal patches.

4.         Pain Relief (Analgesic Effect) :

It is well known that coriander has minor pain-relieving effects. Because of this, it is a good option for buccal patches that are meant to relieve oral pain, whether it be from dental discomfort, mouth ulcers, or the healing process following surgery.

5.         Supporting Drug Absorpton :

According to certain research, coriander might help enhance the way certain medications are absorbed through mucosal membranes. This characteristic may help buccal drug delivery systems by increasing the bioavailability of drugs taken through this route.

6.         Other :

Aromatic, carminative, stimulant, alterative, antispasmodic, diaphoretic and flavouring agent. It is also used as refriger-ant, tonic, appetizer, diuretic, aphrodisiac, and stomachic. Coriander can be applied externally for rheumatism and painful joints. The infusion of decoction of dried fruit of cardamom is useful for the treatment of sore-throat, indigestion, vomiting, flatulence, and other intestinal dis-orders.

 •          Turmeric :

Synonyms : Saffron Indian; haldi (Hindi); Curcuma; Rhizoma cur-cumae.

Biological Source : Turmeric is the dried rhizome  of Curcuma  longa Linn. (syn. C.domestica Valeton)., belonging to family Zingiberaceae.

Chemical Constituents : Turmeric contains yellow colouring matter called as curcuminoids (5%) and essential oil (6%). The chief constituent of the colouring matter is curcumin I (60%) in addition with small quantities of curcumin III, curcumin II and dihydrocurcumin. The volatile oil contains mono- and sesquiterpenes like zingiberene (25%), α-phellandrene, sabinene, turmerone, arturmerone, borneol, and cineole. Choleretic action of the essential oil is attributed to β-tolylmethyl carbinol.

The volatile oil also contains α- and β-pinene, camphene, limonene, terpinene, terpinolene, caryophyllene, linalool, isoborneol, camphor, eugenol, curdione, curzerenone, curlone, AR-curcumenes, β-curcumene, γ-curcumene. α- and β-turmerones, and curzerenone[9].

Uses :

1.         Anti-inflammatory Properties:

Curcumin, the active compound in turmeric, is renowned for its ability to reduce inflammation. Buccal patches offer a direct way to apply turmeric to the mucosal tissues of the mouth, providing targeted relief in conditions such as[10]:

•           Oral Mucositis: A painful condition marked by inflammation in the mouth’s lining, often caused by chemotherapy or radiation. Curcumin’s anti-inflammatory effects can help alleviate pain and promote healing.

•           Gingivitis or Periodontitis: These gum diseases, which cause swelling and irritation of the gums, may be alleviated by curcumin’s ability to reduce inflammation and fight infection.

2.         Pain-Relieving Effects:

Turmeric’s natural analgesic properties can be beneficial for easing various types of oral pain. A buccal patch could provide concentrated, localized relief for conditions like:

•           Oral Pain from Ulcers or Injuries: Curcumin can help reduce discomfort from mouth ulcers or oral wounds by soothing the affected area.

•           Toothaches: The anti-inflammatory and pain-relieving nature of turmeric can offer comfort for tooth-related pain.

•           Sore Throat: When the throat is inflamed, curcumin’s pain-relieving properties may help reduce irritation and discomfort.

3.         Antioxidant Benefits:

Curcumin is a potent antioxidant that helps protect cells from damage caused by oxidative stress. By using a buccal patch, the turmeric can deliver these protective benefits directly to the oral tissues, which may assist in :

•           Post-Dental Healing: After dental treatments or oral injuries, curcumin may aid in healing by reducing oxidative stress and promoting tissue regeneration.

 •          Protection Against Free Radicals: By neutralizing free radicals, turmeric helps

maintain the integrity of oral tissues, preventing long-term damage and supporting overall oral health.

4.         Antibacterial and Antifungal Properties:

Turmeric has been shown to have antibacterial and antifungal effects. A buccal patch containing turmeric could be used to:

•           Combat oral infections caused by bacteria or fungi (e.g., Candida infections)

•           Help in preventing plaque formation and reducing bad breath

5.         Treatment Mouth Ulcers:

Turmeric's natural healing properties can be used in a buccal patch to help with the healing of mouth ulcers or canker sores, reducing the time it takes for them to heal while also reducing associated pain and inflammation[11].

6.         Other :

Turmeric is used as aromatic, antiinflammatory, stomachic, uretic, anodyne for billiary calculus, stimulant, tonic, car minative, blood purifier, antiperiodic, alterative, spice, colouring agent for ointments and a common household remedy for cold and cough. Externally, it is used in the form of a cream to improve complexion. Dye-stuff acts as a cholagogue causing the contraction of the gall bladder. It is also used in menstrual pains.

Curcumin has choleretic and cholagogue action and is used in liver diseases. Curcumin is

a nontoxic authorized colour, heat resistant and sensitive to changes in pH. Curcuminoids have antiphlogistic activity which is due to inhibition of leukotriene biosynthesis. ar- Turmerone has antisnake venom activity and blocks the haemorrhagic effect of venom.

EVALUATION PARAMETERS OF MUCOADHESIVE BUCCAL PATCH –

1.         Appearance:

The formulated buccal patches visually observed for their color. Also Visual checks for color, clarity, flexibility, texture, appearance and odor were made on each created patch[12].

2.         Surface texture:

By simply touching the surface of the formulated buccal patch the surface texture can be evaluated.

3.         Thickness uniformity:

The thickness of each patch is measured by using digital vernier callipers at five different positions of the patch and the average is calculated.

4.         pH

Surface pH The surface pH of the buccal not entirely set in stone to explore the chance of any in-vivo side effects. Since an essential or acidic pH can disturb the buccal mucosa, keeping the surface pH as close is basic to nonpartisan as could really be expected. A consolidated glass cathode was utilized for this reason. The buccal patches were kept in touch with 1

ml of refined water (pH 6.5 ± 0.05) and permitted to grow for two hours at room temperature also, pH was noted somewhere around acquiring the cathode contact with the outer layer of the fix and permitting it to equilibrate for 1 moment[13].

5.         Folding Endurance

The folding endurance of each patch is determined by repeatedly folding the patch at the same place till it is broken or folded up to 300 times, which is considered satisfactory to reveal good film properties[14].

6.         Swelling study

Buccal patches are weighed individually (designated as W1), and placed separately in 2% agar gel plates, incubated at 37°C ± 1°C, and examined for any physical changes. At regular 1hour time intervals until 3 hours, patches are removed from the gel plates and excess surface water is removed carefully using the filter paper 18,19[15-16].

RESULT AND DESCUSSION[17-18] –

IDENTIFICATION TEST:

EVALUATION TEST-