Formulation and Evaluation of Vaginal Suppository using Nelumbo Nucifera for Hormone Imbalance Management

Suppositories are specially shaped, solid dosage forms of a medicament intended for insertion into body cavities other than the mouth, where they melt, or dissolved in the cavity fluids to release the medicament and exert a localized or systemic effect. The suppository is design for local effects like antiseptic, antifungal etc, The suppositories are available in different weights, sizes and shapes. The suppository must dissolve in the body cavity fluids to release medicament. The     medicament is incorporator into a suppository base.

TYPES OF SUPPOSITORY:

Different types of suppositories are available in various size and     shapes.

• Rectal suppository
• Vaginal suppository
• Urethral suppository
• Nasal suppository
• Ear suppository         

Fig no 1: Vaginal suppository

VAGINAL SUPPOSITORY:

• A vaginal suppository is a medicated solid form, typically bullet-shaped or ovular, designed to be inserted into the vagina.
• It's used to deliver medication directly to the vaginal tissues. 
• A vaginal suppository is a small, solid medication inserted into the vagina to treat various conditions like infections, hormone imbalances, or birth control. It's designed to dissolve or melt within the vaginal cavity, releasing the medication to act locally. 
• A vaginal suppository provides targeted relief from conditions affecting the vagina. They also tend to be fast acting due to their rapid absorption. It is important to follow a doctor’s advice when using vaginal suppositories. They can advise on safety of use.
• The term "Lotus Leaf Vaginal Suppository" appears to be used in reference to vaginal suppositories containing Lotus (Nelumbo nucifera) leaf extract as a key ingredient. These suppositories are promoted for their potential to address various vaginal health.

Fig no 2: vaginal cavity

USES:

• Treatment of Vaginal Infections: They may help treat vaginal infections like bacterial vaginosis (BV) and yeast infections.
• Maintaining Vaginal pH Balance: Ingredients like lactic acid may contribute to restoring and maintaining the natural acidic vaginal environment (pH 3.8-4.5) to inhibit harmful bacterial and fungal growth.
• Addressing Symptoms: They may help alleviate associated symptoms such as vaginal itching, burning, odor, and abnormal discharge. 

ADVANTAGES OF SUPPOSITORY:

• Does not cause nausea and vomiting due to gastric irritation in case of oral therapy
• Used before surgery since oral therapy is restricted
• Can be administered to unconscious patients
• Can be used as targeted drug delivery system
• Get to site of action with lower dose reducing systemic toxicity
• Highly beneficial in haemorrhoids or vaginal infections
• Prolonged drug action achieved
• Suppositories dissolves faster
• Total bioavailability achieved
• No need of applicator
• Non staining
• Non itching

DISADVANTAGES OF SUPPOSITORIES:

• Mucosal irritation
• Patient compliance
• Erratic and undesired absorption
• Placement too high into rectum may lead to first pass metabolism
• Installation may trigger defecation reaction
• GI state affects absorption:
• Diarrhea& disease states affect absorption

HORMONES:

Hormones are our bodys  chemical messengers. The travel in our bloodstream to    tissues or organs. They work slowly ,overtime ,and affect many different processes, techniques.

• • • Growth and development
    • Metabolism­­-how your body gets energy from the foods you eat
    • Sexual function
    • Reproduction

Endocrine gland, which are special groups of cells, make hormones. The major endocrine glands are the pituitary, pineal, thymus, thyroid, adrenal glands, and pancreas. In addition, men produce hormone in there and women produce them in their ovaries.

AIM OF THE WORK         

The main aim of this project is to formulate and evaluate the efficacy of a vaginal suppository of nelumbo nucifera for regulating hormones by extended release, particularly in addressing the estrogen level.

Hormone related issues e.g:

• Polycystic ovary syndrome[PCOS]
• Menstrual irregularities
• Thyroid disorder
• Estrogen –progesterone imbalance
• Androgen –related disorders

OBJECTIVES:

• To investigate the phytochemical constituents of nelumbo nucifera responsible for its hormone regulatory effects.
• To formulate and optimize a vaginal suppository of nelumbo nucifera with enhanced bioavailability by extended release.
• To evaluate the in vitro efficacy of the formulate vaginal suppository in regulating hormonal balance.
• To assess the safety and tolerability of the vaginal suppository in health patients.
• To enhance the solubility of nelumbo nucifera by adding the polymer of PEG4000

IV. PLAN OF WORK

V. PLANT PROFILE

Medicinal plants have been a major source of therapeutic agents since ancient times to cure human disease. The revival of interest in natural drugs started in last decade mainly because of the wide spread belief  that green medicine is healthier than synthetic products .Now- a- days ,there is manifold increase in medicinal plant –based industries due to the increase in the interest of use of medicinal plants throughout the world which are growing at a rate of 7-15%annualy .Despite the major advances in the model medicine ,the development of new drug  from natural products is still considered important.

Traditional therapeutics based on herbal  medicinal plant principles is time tested and widely  accepted across various cultural and socioeconomic strata .However ,there is lack of precise guidelines to study the herbal compounds and till date a very meagre portion of this tremendous potential drug –repertoire has been scientifically screened .Hence ,there is a real need for scientific evidence-based validation of these agents .

Fig no 3: Lotus leaf

CHEMICAL TEST FOR QUERCETIN:

TABLE NO: 1

Fig no: 4 Chemical testes for Nelumbo nucifera (lotus)

FORMULATION:

The soxhlet extraction process is a laboratory technique that uses soxhlet extractor to extract compounds from solid materials of nelumbo nucifera.

Fig no:5

1. Prepare the apparatus;

Place the solid sample of nelumbo nucifera and water 1:10 in a thimple – shaped filter paper,and position it in the soxhlet extractor . Connect the condenser to a cold –water source using rubber tubing.

2. Heat the solvent :

Use a heating mantle to heat the solvent in a round bottom flask. The temperature should be regulated based on the boiling point of the solvent.

3. Extract the compound:

The solvent vapours come into contact with the extractant, and the solvent is boiled and condensed. The condensed solvent drops back into the thimble, washing the sample.

Preparation of suppository:

Fusion Molding involves first melting the suppository base, and then dispersing or dissolving the drug in the melted base. The mixture is removed from the heat and poured into a suppository mold. When the mixture has congealed, the suppositories are removed from the mold. The fusion method can be used with all types of suppositories and must be used with most of them.

Suppositories are generally made from solid ingredients and drugs which are measured by weight. When they are mixed, melted, and poured into suppository mold cavities, they occupy a volume – the volume of the mold cavity. Since the components are measured by weight but compounded by volume, density calculations and mold calibrations are required to provide accurate doses.

When a drug is placed in a suppository base, it will displace an amount of base as a function of its density. If the drug has the same density as the base, it will displace an equivalent weight of the base. If the density of the drug is greater than that of the base, it will displace a proportionally smaller weight of the base. Density factors for common drugs in cocoa butter are available in standard reference texts. The density factor is used to determine how much of a base will be displaced by a drug. 

TABLE NO :2

Fig no: 6

RESULT AND DISCUSION

I. PREFORMULATION STUDY

Organoleptic evaluatin of  ( API)

API greenish powder, light, green, vegetable-like aroma, fresh and elegant.

II. ANALYTICAL DEVOLPMENT:

The FTIR absorption spectra of the nelumbo nucifera were taken in the range 4000-500 using KBR disc method the major peakes were reported evaluation of purity.

1. FTIR SPECTRA OF NELUMBO NUCIFERA

Fig no7

2. DRUG-EXCIPIENT COMPATIBILITY

FTIR Compatiblity study

Excipient compatibility was determined using FTIR spectroscopy; the prepared nelumbo nucifera extract and final blend were subjected to FTIR study.

Fig no 8

DISCUSSION

FTIR spectrum of API showed the characteristic functional group of drug along with their wave numbers.

Result indicates that , there is no interaction between and Excipient used in the formulation

3. EXCIPIENT COMPATIBILITY

Fig no 9

TABLE NO :6

DRUG- EXCIPIENT COMPATABLITY FTIR

COMPATIBILITY STUDY

The FTIR spectroscopy is used to determine the drug  excipient compatibility.suppository FTIR spectra or result were tabled above,

DISCUSSION

The characteristic functional group of drugs along with wave numbers were showed the FTIR spectrum API of nelumbo nucifera . Based upon the above IR reports of drugs and polymer compatible studies the must the functional group are same.

Results indicates that,there is compatibility between the drug and excipient used in the formulation .The main functional group of nelumbo nucifera (-OH group)  

FORMULATION TABLE

TABLE NO :7

UV SPECTROSCOPIC ANALYSIS

CONCENTRATION OF CALIBRATION CURVE OF NELUMBO NUCIFERA

The λ max of NELUMBO NUCIFERA is 254nm

Fig no 10

DISCUSSION

The λ max Nelumbo nucifera is 254nm

The absorbance of nelumbo nucifera wuth stimulated concentrations are tabulated below.

Vaginal cavity and 0.1N Hcl in different concentrations are tabulated below.

DISINTEGRATION ABSORBENCE VALUE OF TABLET IN 0.1N HCL:

TABLE NO: 8

FIG NO : 9

DISINTEGRATION

ABSORBENCE OF VAGINAL SUPPOSITORY (PH4.5)

TABLE NO: 10

FIG NO :12

DISSOLUCTION

ABSORBENCE OF VALUE OF 0.1N HCL

TABLE NO : 11

FIG NO :13

DISSOLUTION

ABSORBENCE OF VAGINAL SUPPOSITORY (PH 4.5)

TABLE NO: 12

FIG NO : 13

FORMULATION AND EVALUATION OF VAGINAL SUPPOSITORY 

TABLE NO :13

1) Uniformity of weight:

TABLE NO: 14

2) Thickness :

Vaginal suppositories are typically manufactured with a thickness (diameter) ranging from about 10 to 15 millimeters.This size is designed to balance patient comfort with adequate drug load and structural integrity.

3) Surface pH:

FIG NO :15

4) Disintegration test

The disintegration test for a Nelumbo nucifera (lotus) suppository is conducted to ensure it melts or disperses within a specified time at body temperature (36–37°C), adhering to pharmacopoeial standards for molded suppositories.

FIG NO :16