K.V.N. Naik S.P. Sanstha’s, Institute of Pharmaceuticals Education & Research, Canada Corner, Nashik, India.
The main objective of any drug delivery technique is to appropriately distribute the medication to the body, but patient compliance must also be taken into account. Fast-dissolving drug delivery technologies, such as Orodispersible Films (ODFs), make it easy to administer medication to both the general public and specific demographic groups that have trouble swallowing, like children and the elderly. ODFs are innovative dosage forms that decompose and dissolve in the mouth. Intra-oral absorption lowers the unit dose required to achieve the intended therapeutic effect by encouraging rapid action and preventing first-pass effects. One innovative and promising oral delivery method is orodispersible films. ODFs have previously been extensively researched and demonstrated to be suitable for this formulation strategy, such as when delivering API nanoparticles.
Oral medication delivery is the most commonly used and patient-friendly method. Most patients—adults, children, and geriatric patients—take their prescriptions as tablets or capsules . Firm gelatin tablets and capsules, however, are not easy for 26–50% of patients to swallow . These patients mainly include geriatric patients who cannot swallow conventional oral dosage forms because of trembling of hands and dysphagia, pediatric patients who generally avoid taking solid oral dosage forms because of their underdeveloped nervous and muscular systems, mentally ill and developmentally disabled individuals, and uncooperative patients who are put on reduced liquid intake schedules, feel nausea, or are on the go without access to water. The pharmaceutical industry is increasingly interested in orodispersible systems . These systems generally melt or disintegrate within less than a minute, therefore chewing or water is often not required. Compared to oral administration, these technologies offer better clinical profiles due to the possibility of mucosal absorption. Recently, thin films which rapidly dissolve or disintegrate in the buccal cavity have been suggested. Mouth-dissolving films are new dose forms which melt or dissolve in the oral cavity. These are extremely thin pharmaceutical excipients, about the size of a postage stamp. These dosage forms are applied to any mucosal tissue, including the tongue . The films immediately hydrate and adhere to the site of application with the help of saliva. Because of its rapid dissolving nature, with minor modifications, it can also deliver the drug for oral GIT absorption.
Orodispersible Film
Orodispersible films are single or multilayer sheets created of the suitable materials that are meant to promptly release the loaded active component in the mouth, forming a thin suspension or solution in the saliva without mastication or water intake. These orodispersible films are created in such a way that water is not necessary for administration since they immediately break apart within a few seconds, releasing the medication into the mouth. When placed on the tongue, orodispersible films quickly hydrate by soaking up saliva after the dosage form's actie medicinal ingredient disintegrates and/or dissolves. This thin films come in a range of sizes and shapes. They dissolve and release quickly, and they have excellent mucoadhesion. These movies are excellent for patients who are bedridden, emetic, experiencing diarrhoea, an allergic attack, or coughing and lead an active lifestyle. They are also useful for youngsters, the elderly, and patients who are pediatric or geriatric. Additionally, it is helpful for targeted actions such local anesthesia for toothaches, oral ulcers, or teething .
Clinical Application and Prospective Developments:
ODF can be utilized for localized treatment within the mouth, including local anesthesia during dental work, as well as for bacterial or fungal infections, and conditions like sore throats, oral ulcers, pharyngitis, and tonsillitis . ODF offers numerous benefits that render it highly effective in emergencies and for patients with schizophrenia and dysphagia. ODFs created with small molecules were effectively developed for both local and systemic effects. Table 5 provides a concise summary of the active and finished clinical trials for various drug-loaded ODFs designed for oral administration. In 2010, the FDA authorized the first prescription ODF named Zuplenz, featuring ondansetron as the active ingredient. Numerous prescription and over-the-counter ODFs have received approval since that time and have achieved substantial worldwide popularity. Nonetheless, numerous formulation challenges persist, with the two primary issues being unappealing-tasting medications and their elevated dosages. The application of ODFs for nanoparticle delivery has been extensively researched
Advantages
Drawbacks :
It is not possible to add a higher dose to these ODFs, unlike oral dissolving tablets.
Longer preservation is troublesome due to its hygroscopic nature and the necessity for specialized packaging.
Giving drugs that are unstable at buccal pH is forbidden.
A long-time of abstinence from food and liquids following the consumption of ODFs.
These films are made with more expensive techniques than oral dissolving tablets.
Methods of preparation
1. Solvent casting method:
Solvent casting is one of the oldest methods used to prepare films. Orodispersible films are prepared by using this method. This method is applied for the preparation of film of size 2x2 cm and 3x2 cm. In this, drug and all components are taken in either organic or aqueous solvent according to selection, and mixed with and stirred.
dissolve water-soluble polymers. Once carefully cast, it is left to dry on the surface of a glass, Teflon, or any other proper material petri dish or plate. The solution is spread on an inert base with special equipment developed for bulk production with the use of rollers. The trapped air is removed by vacuum. The penultimate step is the drying of films and the evaporation of residual solvent in order to obtain the final product. After the drying of the films, they are cut, peeled, and packaged.
2. Method of semisolide casting
First, a water-soluble polymer film-forming solution is made. This solution is then transferred to an acid-insoluble polymer solution, which can be made by mixing cellulose acetate butyrate or cellulose acetate phthalate in a roughly 1:4 ratio with either a sodium hydroxide solution or an ammonium hydroxide solution. Plasticizer is then carefully added to form a gel mass that may be shaped into thin films.
3. Hot-melt Extrustion
This method can be utilized drawing from the expertise of the plastics sector, where formulators are capable of extruding a blend of drugs, polymers, and relevant excipients into preferred final forms to establish suitable drug-release characteristics. Twin screw extruders are beneficial in pharmaceutical formulations as they can uniformly and consistently mix different formulation materials, improving bioavailability and dissolution rate. API is combined with other components in a dry form, heated until the blend becomes molten, and then extruded to create thin films. Using the appropriate approach, the solvent is entirely eliminated.
4. The Rolling Method
In this process, a suspension or solution comprising of the drug is applied onto the carrier. The common primary solvents used are water and mixture of alcohol and water. After drying on the heated surface, the films are cut into required shapes and sizes by rollers. Additional chemicals such as API, polymer, plasticizer, and all the other required chemicals are mixed in small quantities of aqueous solvent using high-shear processor.
FORMULATION OF ORODISPERSIBLE FILM:
These are the elements that were employed in the preparation:
Table 1: The general formulation of ODF film
|
Component |
Drug |
Polymer |
Plasticizers |
Saliva stimulants |
Super disintegrant |
Flavouring agents |
Sweeteners |
Colouring agents |
|
Concentration (w/w) |
1-25% |
40-50% |
0-20% |
2%-6% |
0%-8% |
Q.s |
3%-6% |
Q.s |
Active Pharmaceutical Ingredients:
API can be provided via any medication category that can be taken orally or through the buccal mucosa. In orodispersible films, the active pharmaceutical ingredient (API) is typically present at a concentration ranging from 1 to 50% w/w; nonetheless, for the formulation to work effectively, the API should be micronized to improve its texture, homogeneity, and dissolution rate.movie that is orodispersible. Antiemetics, neuroleptics, analgesics, antihistamines, sedatives, hypnotics, diuretics, antibacterial agents, cardiovascular medications, and erectile dysfunction treatments are some of the drug categories that may be utilized to create orodispersible films.
Table 2: List of drugs that can be incorporated in orodispersible film
|
Sr. No. |
Name of Drugs |
Dose (mg) |
Therapeutic use |
|
1. |
Azatadine Maleate |
1 |
Anti-histaminic |
|
2. |
Azelnidipine |
4 |
Anti-hypertensive |
|
3. |
Nicotine |
2 |
Smoking cessation |
|
4. |
Loperamide |
2 |
Anti-diarrhoeal |
|
5. |
Ondansetron |
2.5 |
Anti-emetic |
|
6. |
Triprolidine hydrochloride |
2.5 |
Anti-histaminic |
|
7. |
Zolmitriptan |
2.5 |
Anti-migraine |
|
8. |
Salbutamol |
4 |
Anti-histaminic |
|
9. |
Chlorpheniramine Maleate |
4 |
Anti-allergic |
|
10. |
Cetirizine |
5-10 |
Anti-histaminic |
|
11. |
Acrivastine |
8 |
Anti-histaminic |
|
12. |
Loratadine |
10 |
Anti-histaminic |
|
13. |
Omeprazole |
10-20 |
Proton pump inhibitor |
|
14. |
Famotidine |
10 |
Antacid |
|
15. |
Ketoprofen |
12.5 |
Analgesic |
|
16. |
Dicyclomine hydrochloride |
25 |
Muscle relaxant |
|
17. |
Diphenhydramine hydrochloride |
25 |
Anti-allergic |
|
18. |
Sumatriptan succinate 35- |
35-70 |
Anti-migraine |
Film forming polymers :
The selection of polymer is the most critical and detrimental element for the effective production of oral dissolving films, since the tensile strength of the films depends on the kind of polymer chosen. I apologize, but it appears that your submission doesn't contain any text to paraphrase. Could you please provide the text you'd like me to work with? Mouth dissolving films are based on polymers. The entire polymer used is water soluble, as it rapidly breaks down and imparts strong mechanical properties along with pleasant mouthfeel effects to the films . Synthetic and natural polymers may be used separately or together with other polymers to achieve the desired film properties.
Plasticisers :
Plasticizers are used to provide flexibility or elasticity to materials, improving automated film holding characteristics such as tensile strength and expansion of the MDFs. Plasticizers reduce the brittleness of MDFs by improving the durability of the polymer. The choice of plasticizers relies on their compatibility with the polymer, drug, and other excipients.Glycerol serves as a superb plasticizer for films made from PVA. HPC and PVA films both incorporate polyethylene glycol (PEG).
Saliva stimulating vehicles :
The aim of using a saliva bracing agent includes enhancing saliva production, as this will accelerate the disintegration rate of MDFs within the oral cavity. Overall, food-safe acids may serve as stimulants for saliva production.
Sweetening vehicles :
Pharmaceutical medications that are intended to dissolve or break apart in the mouth now include a sweetener as a key component similar to food items. Sweetening agents mitigate the harsh flavor of the medications.
Flavoring vehicles:
The type of medication, the user's age, and their personal preferences are taken into consideration when selecting a flavoring component. Flavor-transporting vehicles can operate alone or in tandem with other vehicles. The ideal ratio for adding flavors to the formulation is 10% w/w.
Coloring automobiles:
The use of color additives in the manufacturing of mouth-dispersing films has received approval from the Food and Drug Administration (FD&C). For example, the amount of color used should not be more than 1% of the formulation's weight. The most widely used coloring agent is titanium dioxide.
Surfactant:
To facilitate the rapid dissolution of the films and the release of the active medicinal ingredient, surfactants are added to improve the wettability, solubility, and dispersibility of the films. Sodium lauryl sulfate, Tween 80, Poloxamer 407, and a variety of other surfactants are among the most frequently used.
CHARACTERIZATION OF ODF FILM:
Orodispersible film analyzed through various assessment methods.
Morphological studies:
Scanning Electron Microscopy, known as SEM, is a robust investigative technique whose capabilities have been extensively recognized in scientific publications for examining and analyzing surface morphology.
Raman spectroscopy with X-ray diffraction:
X-ray diffraction patterns and Raman spectroscopy can be used to determine if APIs incorporated into films in their unprocessed state are crystalline or amorphous.
Thickness measurements:
For the measurement of the thickness of each film, an advanced measuring instrument known as a Vernier calipermicrometer is used. This instrument is designed specifically to measure small distances or sizes, hence providing very accurate and reliable measures.
Resistance to tears:
The tear strength of plastic film or ODF films is a complex characteristic that is closely connected to its overall breakage resistance. The force required to initiate tearing is assessed using a very low loading rate of 51 millimeters (2 inches) per minute.
Variation in weight:
The samples taken for this test are one square centimetre each from five distinguishable and different sites. Each film strip is weighed and recorded individually for accurate and precise measurements to be determined. This makes the process organized, allowing any increase or decrease in weight to be duly identified and noted. This will also allow for complete determinations about the weight variance displayed by the film strips under study.
Transperency:
The transparency of the films can be gauged using a primary UV spectrophotometer. The film samples should be cut into rectangles using a razor blade so that they can be placed inside the spectrophotometer. Measure how well different materials allow light with a wavelength of 600nm to pass through them.
Determination of moisture uptake:
Films are placed in regulated conditions of relative humidity and temperature with specific settings for a week to assess the moisture absorption capacity.
Percentage of weight gain = [(Weight after experiment - Initial weight) / Initial weight] x 100
Drug content determination:
Pharmacopeias serve as official compilations of standards and guidelines through which the quality of pharmaceutical products is assessed; hence, the chosen testing method has to be in conformity with severe scientific procedures and regulatory requirements.
Content homogeneity of drug:
This thorough procedure requires analyzing 20 films in total to ensure complete testing of the homogeneity of the API distribution in the entire lot. Ensuring the quality and homogeneity of pharmaceutical products relies on the adherence to strict specifications with regard to content uniformity. More specifically, it is recommended that the content uniformity be within 85 to 115%, so that an acceptable margin of variability may be considered.
Tensile strength:
The device comprises two clamps, one secured at the upper end and the other movable at the bottom end; this is utilized for measuring the tensile strength. Insert the film sample (sized 0.5 x 3cm) between the two clamps and fasten it securely. Tearing and elongation force calculations are performed accordingly.
Angle measurement of contact:
Goniometer: A goniometer is a vital instrument in surface science and interfacial phenomena; it measures the contact angle formed between a liquid droplet and a solid surface. A specific, premeasured quantity of distilled water is gradually poured over the whole area to saturate the dry film.
In-vitro disintegration time:
By visual inspection, the exact time of in-vitro disintegration is determined objectively in a controlled environment within the laboratory. Notably, exactly 10 milliliters of pure water at 370 degrees Celsius acts as the medium for carrying out the disintegration test in a glass dish. In activating it, the sample film is swirled for a precisely predetermined duration of 10 seconds.
PAKAGING AND STORAGE OF ODF FILM:
The propensity of ODF film to break down rapidly during production and storage necessitated costly packaging solutions. The primary packaging material is commonly recognized as the aluminum bag. The rapid card is a packaging solution created by APR-Labtec solely for ODF films. The packing material must receive approval from the Food and Drug Administration (FDA). The system must exhibit strong resilience to unauthorized access or alteration.
Plastic bags with paper lining:
The lightweight pouch demonstrates significant tamper resistance and environmental awareness.
Individual pouch and aluminum pouch:
The primary pouch utilized for packaging ODF film is aluminum, which is widely acknowledged.
Environmental factors:
Blister card containing several units: The thermoplastic material was utilized for blister packaging.
Barrier films:
The application of high barrier films is essential because some drug formulations are vulnerable to moisture.
Modern Evaluation Parameters:
STABILITY STUDIED OF ODF FILM:
According to the guidelines released by the International Council on Harmonisation (ICH), it has been determined that the stability of orodispersible films can be effectively maintained under specific controlled environmental conditions. These conditions consist of 25°C at a relative humidity of 60% and 40°C at a relative humidity of 75%. The stability of the film was conducted in a stability chamber for a duration of 12 months. At regular intervals of 3, 6, 9, and 12 months, film samples were taken and analyzed for standard parameters.
CONCLUSION
This study offers a comprehensive examination that underscores the innovative nature of orodispersible films as delivery systems for medication. These videos present an innovative approach that shows great potential in the pharmaceutical sector. In recent times, film-based dosage forms have attracted considerable interest in the medical and pharmaceutical fields. These recent formulations have demonstrated significant progress in acceptance rates and patient adherence, ultimately transforming the field of drug delivery techniques. A significant benefit of film-based medications lies in their superior safety and effectiveness, particularly when contrasted with traditional dosage forms. Additionally, the improved safety and effectiveness of film-based medications can be attributed to their distinctive structure and design. These films generally consist of thin, pliable layers that encompass the active pharmaceutical ingredient along with different excipients. In numerous emergency situations, like during allergic reactions and asthma attacks, the administration of particular medications is an urgent necessity. Due to their capacity to respond promptly. These substances, commonly known as emergency drugs, play an essential role in quickly managing and reducing the potentially fatal effects related to these critical situations
REFERENCES
Rutuja Ghotekar, Satyam Deore, Kanchan Jagtap, An Overview: Orodispersible Film [ODF]: A Morden Approach Oral Drug Delivery, Int. J. of Pharm. Sci., 2025, Vol 3, Issue 12, 2055-2064. https://doi.org/10.5281/zenodo.17909440
10.5281/zenodo.17909440
