Fast Dissolving Oral Films Research Articles

Fabrication and Characterisation of Oral Fast-Dissolving Film of Metoprolol Succinate

Introduction: Oral, fast-dissolving films are an excellent alternative. The purpose of adopting the solvent casting approach was to create a compelling oral film. Methodology: HPMC E15 and sodium alginate polymers were chosen based on their compatibility. The produced films were evaluated in terms of organoleptic characteristics, weight, thickness, folding durability, tensile strength, drug content homogeneity, surface pH, disintegration time, and in-vitro dissolution kinetics. Results: Among the formulations, F2 had a disintegration time of 14.2 seconds and a phenomenal drug release of 98% in 5 minutes. As a result, formulation F2 emerged as the best option, demonstrating promising qualities for effective drug delivery. Conclusion: These films are made of thin strips and are easily applied to the tongue or oral mucosal tissue. When they come into contact with saliva, they quickly hydrate and attach, resulting in rapid medicine administration. Fast-dissolving oral films are an excellent alternative for patients who have difficulty swallowing traditional drugs, such as pediatric, geriatric, bedridden, or developmentally impaired people. These films are made of thin strips and are easily applied to the tongue or oral mucosal tissue. When they come into contact with saliva, they quickly hydrate and attach, resulting in rapid medicine administration. other: Nil

Preparation and Characterization of Febuxostat Nanosuspension as Fast Dissolving Oral Film

Background: Quickly dissolved oral films are a widely accepted method of delivering drugs and help patients adhere to treatment regimens. Nanosuspensions (NS) are colloidal dispersions of drug particles with a submicron size, and their large surface area enhances the solubility and dissolution of low-water-soluble drugs. Febuxostat (FXT) is a non-purine xanthine oxidase inhibitor with a low dissolution rate that limits its absorption. Objective: To develop fast-dissolving oral films (FDOFs) containing FXT NS and convert NS into solid dosage forms to ease administration and accelerate drug release. Methods: FXT NS was prepared using Soluplus as a stabilizer and Tween80 as a co-stabilizer through an anti-solvent precipitation technique. We prepared FDOFs using a solvent casting method, utilizing hydrophilic polymers like pullulan, polyvinyl alcohol (PVA), gelatin, and plasticizers like polyethylene glycol (PEG400) and glycerin. The study assessed the film's thickness, weight, folding endurance, drug content, disintegration time, and drug release. We validated the drug's compatibility using FTIR, and conducted a crystallinity study using DSC and X-ray powder diffraction. Results: F4 was the optimized formula prepared using PVA and PEG400. In just three minutes, the F4 dissolution rate increased significantly (99.63% vs. 11.23%) compared to the FXT ordinary film. Also, it had good mechanical properties. Conclusions: FXT NS were successfully loaded into FDOFs with accepted properties.

Reducing Temperature of Fused Deposition Modelling 3D Printing for Linalool Fast Dissolving Oral Films by Increasing Printer Nozzle Diameter

Oral thrush and throat infections can occur in a wide range of patients. Treatments are available; however, resistance to drugs is a major problem for treating oral and throat infections. Three-dimensional printing (3DP) of fast dissolving oral films (FDFs) of linalool oil may provide an alternative solution. Linalool oil FDFs were printed by fused deposition modelling across 1–18 % w/w linalool content range with nozzle diameters of 0.4 or 1 mm at the temperature range of 150 °C-185 °C. The FDFs were evaluated for physicochemical and mechanical properties. Increasing the printer nozzle diameter to 1 mm allowed reducing the printing temperature from 185 °C to 150 °C; consequently, more linalool was quantified in the films with improved content uniformity. The higher linalool content in the films increased the film disintegration time and mechanical strength. FDFs containing 10% w/w linalool showed clear antifungal activity against Candida albicans. Raman spectroscopy suggested linalool separation from excipients at higher temperature printing. Viscoelastic measurements indicated that to achieve printing; the elastic modulus of molten filament needed to be higher than the loss modulus at low angular frequencies. In conclusion, increasing the printing nozzle diameter may avoid loss of the active ingredient by reducing the temperature of the 3DP process.

Development of Vitamin C-Loaded Electrospun Nanofibers of Mixture of Polysaccharides of Pullulan/Xanthan Gum for Fast Dissolving Oral Film Applications.

In this study, polysaccharide-based nanofibrous fast dissolving oral films (FDOFs) were developed using pullulan (PUL) and xanthan gum (XG) via electrospinning. The edible, continuous, and bead-free nanofibers with average diameters ranging from 181.17 nm to 260.84 nm were prepared. The morphological, thermal, mechanical, and water-soluble properties of the nanofibrous FDOFs were characterized. For prospective future applications of the developed PUL/XG FDOFs, a model nutrient of vitamin C (VC) was encapsulated into the FDOFs. The success of VC encapsulation was confirmed by Fourier transform infrared spectroscopy. The encapsulation efficiency of VC was above 85% by ultraviolet-visible spectrophotometer. The amorphous structure of PUL/XG in the nanofibers film was demonstrated by X-ray diffractometer. In addition, the edible FDOFs could dissolve in water within 3 s. The nanofibers film we prepared could be used as nutrient or drug carriers and edible packaging film.

Design and Characterization of Fast-Dissolving Oral Film of Apixaban.

Following the COVID-19 pandemic, microvascular and macrovascular thrombotic problems emerged that required anticoagulants. Apixaban (RN) is a factor Xa inhibitor that treats deep vein thrombosis and the two forms of artery diseases (coronary artery disease and peripheral artery disease). The study objective was to create fast-disintegrating Apixaban Oral Thin Films (OTF) with the help of various super disintegrants to shorten disintegration time and enhance drug release in order to assist patients who have difficulty in swallowing conventional dosage forms and increase bioavailability. OTF was created using the solvent casting method. A 22 factorial design was employed in Design-Expert® software to develop an ideal formula. The optimized film formula pH, drug content, disintegration time, folding endurance, and dissolution rate were estimated, and the film was subjected to a short-term stability study. The optimized formula exhibited a cumulative drug release of 93.47% in 60 sec. The drug's in vitro release pattern shows first-order kinetics and fickian diffusion was the mechanism of drug release. These findings supported that Apixaban OTFs offer a quick release of the medication from the administration site into the systemic circulation.

Fast Dissolving Oral Films: Formulation, Evaluation and Future aspects

Fast dissolving oral film (FDOF) are drug delivery systems of the new days having one of the highest patient compliance, safety and are economical than most other dosage forms. Hydrophilic polymers when used as a vehicle come in contact with water get hydrated and thus allow drug release. Hydrophilic polymers also show an adherence property post hydration. Thus the hydrating and adhering properties of hydrophilic polymers makes it most suitable for producing fast dissolving oral film. Fast dissolving oral films are made to be administered into the buccal cavity of humans as the buccal cavity if having saliva and saliva help to hydrate the films leading to drug release. The buccal cavity in humans has a very high amount of blood supply system thus aids in faster drug entrance into the blood circulation. The fast dissolving oral films are capable of initiating drug release within seconds, without chewing and drinking. The instant bioavailability achieved bypassing the fast pass metabolism also adds as a salient feature. Various compositions of different polymers lead to differences in drug release rate of the films. Polymers such as Hydroxy Propyl Methyl Cellulose; Poly Vinyl Alcohol; Ethyl Cellulose; Sodium Carboxymethyl Cellulose are some common hydrophilic polymers that are used to produce fast dissolving oral films. Solvent casting; semi solid casting; hot melt extrusion; solid dispersion extrusion are some common methods of production of fast dissolving oral films. Immediate onset of action in a shorter period with improved bioavailability marked fast dissolving oral film, a dosage form of choice.

Formulation and Evaluation of Fast-Dissolving Oral Film of Rivaroxaban

Formulation and Evaluation of Fast-Dissolving Oral Film of Rivaroxaban

A REVIEW ON FAST-DISSOLVING ORAL FILM

Due to their increased comfort and flexibility, fast-dissolving oral films are the most cutting-edge oral solid dose form. It increases the effectiveness of APIs by dissolving in the oral cavity in under a minute after coming into touch with less saliva than fast-dispersing tablets, without chewing, and without the requirement for water for administration. Some patients, especially those who are young or elderly, have trouble chewing or swallowing solid dose forms. The fear of choking prevents many young and geriatric patients from taking these solid preparations. Consequently, orally dissolving pills have been developed. Due to consumer demand for a fast-dissolving product over conventional tablets or capsules, OTFs have gained a position as an alternative in the market. Depending on the film thickness and choice of the polymer matrix, these films can be adjusted to release the medicine more gradually. These films typically disintegrate in seconds to release the active ingredients. When a dosage form is placed on the tongue or in the oral cavity, it can swiftly hydrate, adhere, and dissolve, allowing for rapid local or systemic drug delivery. This type of dosage form is referred to as a film or strip.

Formulation and Characterization of Montelukast Sodium Mouth Dissolving Film Using Cress Seed Mucilage

There is a rising interest in the development of orodispersible films (ODFs) as an alternative to fast dissolving tablets which is attributed to their faster dissolution rate, higher durability, and better patient compliance. Owing to its rheological and also various functional properties, many researchers tried to discover some of the pharmaceutical applications of L. sativum in the development of various dosage forms, in addition to its therapeutic studies, such as binding, dissolving, gelling and sustained release dosage form. The fast-dissolving oral film of the Montelukast sodium by using Cress seed mucilage (CSM) and HPMC (15cps) is prepared by solvent casting method. The fast-dissolving oral film evaluated for folding endurance, surface pH, in-vitro disintegration time, drug content and in-vitro drug release. The physical appearance and folding endurance properties were found to be reasonably good and electron microscopy shows that films are clear, colorless with smooth surface.The drug content of all the films was in the range suggesting that drug was uniformly dispersed throughout all films. The present study was an attempt to develop and evaluate an oral fast dissolving drug delivery system using cress seed mucilage as a film former.
 Keywords: Orodispersible film, Montelukast sodium, Cress seed mucilage, HPMC

FORMULATION, DEVELOPMENT AND EVALUATION OF FAST DISSOLVING ORAL FILM OF AMLODIPINE

FORMULATION, DEVELOPMENT AND EVALUATION OF FAST DISSOLVING ORAL FILM OF AMLODIPINE

The Use of Micro-Ribbons and Micro-Fibres in the Formulation of 3D Printed Fast Dissolving Oral Films

Three-dimensional printing (3DP) allows production of novel fast dissolving oral films (FDFs). However, mechanical properties of the films may not be desirable when certain excipients are used. This work investigated whether adding chitosan micro-ribbons or cellulose microfibres will achieve desired FDFs by fused deposition modelling 3DP. Filaments containing polyvinyl alcohol (PVA) and paracetamol as model drug were manufactured at 170 °C. At 130 °C, filaments containing polyvinylpyrrolidone (PVP) and paracetamol were also created. FDFs were printed with plain or mesh patterns at temperatures of 200 °C (PVA) or 180 °C (PVP). Both chitosan micro-ribbons and cellulose micro-fibres improved filament mechanical properties at 1% w/w concentration in terms of flexibility and stiffness. The filaments were not suitable for printing at higher concentrations of chitosan micro-ribbons and cellulose micro-fibres. Furthermore, mesh FDFs containing only 1% chitosan micro-ribbons disintegrated in distilled water within 40.33 ± 4.64 s, while mesh FDFs containing only 7% croscarmellose disintegrated in 55.33 ± 2.86 s, and croscarmellose containing films showed signs of excipient scorching for PVA polymer. Cellulose micro-fibres delayed disintegration of PVA mesh films to 108.66 ± 3.68 s at 1% w/w. In conclusion, only chitosan micro-ribbons created a network of hydrophilic channels within the films, which allowed faster disintegration time at considerably lower concentrations.

Central Composite Design for the Development of Trimetazidine Dihydrochloride-Loaded Fast Dissolving Film

A fast-dissolving dosage form is an approach used to improve therapeutic efficacy and bioavailability by avoiding the first-pass metabolism of the cargo. Besides, the approach causes rapid cargo absorption from the pre-gastric area which may outcome in the quick inception of action. The trimetazidine dihydrochloride (TDC) is an anti-anginal drug and there is a prerequisite to provide fast onset of action to treat angina. Therefore, the present work was aimed to prepare and evaluate fast-dissolving oral films (FDOF) of TDC to provide fast onset of action. The FDOF is prepared by using the solvent casting method and it was optimized by employing a central composite statistical design. The two independent variables such as HPMC K4M and PEG 400 are the film-forming polymers which are evaluated at three levels. The dependent variables selected as folding endurance, disintegration time, and % drug release. The formulation was prepared and optimized the batch F-4 showed the least disintegration time (19 s) and the highest drug release (98.55±7.90%). Moreover, the ex-vivo mucus permeation study showed better permeation and satisfying physicochemical properties. As per the above results, we conclude that the prepared formulation could be a novel dosage form to improve drug delivery and patient compliance.

The Optimization and Evaluation of Flibanserin Fast-Dissolving Oral Films.

Flibanserin (FLB) is a drug used for female hypotensive sexual desire disorder approved by the FDA in August 2015. FLB exhibits extensive hepatic first-pass metabolism and low aqueous solubility, hence poor oral bioavailability. In this study, beta hydroxypropyl cyclodextrin-FLB inclusion complexes were incorporated into orally fast dissolving films. This dosage form was expected to improve FLB aqueous solubility, which would give fast onset of action and decrease presystemic metabolism, hence improving oral bioavailability. The inclusion complex at a ratio of 1:1 was prepared by the kneading method. Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), and powder X-ray diffractometry (XRD) were used to confirm complex formation. The Box–Behnken design (15 different formulae of FLB fast-dissolving oral films (FLBFDOFs) were utilized for the optimization of the prepared films. The Expert Design 11 program was utilized to examine the effects of three selected factors, polymer concentration (X1), plasticizer concentration (X2), and disintegrant concentration (X3) on four responses: disintegration time (DT), initial dissolution rate (IDR), dissolution efficiency (DE), and film quality (QF). Numerical optimization was performed by minimizing disintegration time (Y1), while maximizing the initial drug dissolution rate (Y2), dissolution efficiency (Y3), and the quality factor (Y4). The statistical analysis showed that X1 has a significant positive effect on the disintegration time and a significant negative effect on IDR. While X2 and X3 produced a nonsignificant negative effect on IDR. Dissolution efficiency was maximized at the middle concentration of both X2 and X3. The best film quality was observed at the middle concentration of both X1 and X2. In addition, increasing X3 leads to an improvement in film quality. The optimized film cast from an aqueous solution contains hydroxypropyl cellulose (2%) as a hydrophilic film-forming agent and propylene glycol (0.8%) as a plasticizer and cross povidone (0.2%) as a disintegrant. The prepared film released 98% of FLB after 10 min and showed good physical and mechanical properties. The optimized formula showed a disintegration time of 30 s, IDR of 16.6% per minute, DE15 of 77.7%, and QF of 90%. This dosage form is expected to partially avoid the pre-systemic metabolism with a fast onset of action, hence improving its bioavailability that favors an advantage over conventional dosage forms.

Development and In vitro characterization of pullulan fast dissolving films loaded with Panax ginseng extract, antioxidant properties and cytotoxic efficiency on lung and breast cancer cell lines

The objectives of the current research were to produce fast dissolving oral films (FDOFs) containing standardised freeze-dried ginseng root extract (FDG) and to exploit and evaluate the effect of pullulan on the fast-dissolving oral films to impart desirable features to the drug formulation, such as rapid drug release, high release rates and improve the active ingredients' stability. Pullulan was used as a film-forming polymer and propylene glycol as a plasticizer, and films were produced by a solvent-casting method. The FDOFs were evaluated for the physicomechanical properties such as disintegration, Young's modulus, tensile strength and elongation at the break. The interaction between the polymer and freeze-dried ginseng extract in the film formulation was determined by ATR-FTIR method. Morphological characteristics were identified by scanning electron microscopy. Along with the formulation study, its antioxidant capacity and anti-cancer effect on lung and breast cancer cell lines were also observed. In different antioxidant experiments (FRAP, CUPRAC, DPPH and ABTS), the total antioxidant content of FDG was observed to be between 3.379 and 11,216 mg/g extract. In the present study, we also tested FDG extract on human breast cancer model MCF-7 and human lung cancer model A549 cell lines in vitro. Based on MCF-7 and A549 cell viability results, FDG extract exerted cytotoxicity on both cancer lines in a dose-dependent manner. The results manifested that the FDOFs containing FDG had good physicomechanical properties and fast release profiles. The incorporation of the FDG into the films promoted reduction of the tensile strength and Young's modulus, and an increase in elongation compared to F1. The film exhibited maximal release in 10 min of the active compounds (Rb1 and RG2), and it was more than 97 ± 0.35%. The results may lay the groundwork for future studies, regarding the development of FDOFs as P. ginseng extract-based dosage forms, which might increase the pharmacological activity and multifunctional properties closer to the desired level and may be a useful and effective anticancer-containing product with future in vivo studies.

Optimization of curcumin nanofibers as fast dissolving oral films prepared by emulsion electrospinning via central composite design

The pharmacological beneficial effects of curcumin (CUR) are compromised by its water insolubility, poor bioavailability, and instability. The fast-dissolving oral films prepared by hydrophilic biodegradable polymers can be used to address this issue. This study aimed to application of emulsion-electrospinning to fabricate the CUR-loaded PVPK90 nanofibers. The nanofibers were prepared using the central composite design. The selected variables were drug concentrations, flow rates, acetone content, and organic phase percentages and the evaluated responses were diameters, loading %, wetting and disintegration times. The fabricated nanofibers were also subjected to DSC, FTIR, XRD, TEM, SEM and fluorescence microscopy analyses, as well as drug release assessment. The formulation containing 6 mg/mL CUR, 30% organic phase, 0.4 mL acetone, with the flow rate of 1 mL/h was selected as the optimum formulation. The results confirmed the formation of uniform bead-free nanofibers. The nanofibers prepared in the optimum condition showed a good flexibility, short wetting and disintegration times, as well as an amorphous structure. The drug release pattern indicated the rapid release of the drug within 30 s. Our findings confirmed that the O/W emulsion electrospinning-based PVPK90 nanofiber would be beneficial as a fast dissolving oral film for dissolution enhancement of curcumin.

Fast-dissolving oral films containing dextromethorphan/phenylephrine for sinusitis treatment: formulation, characterization and optimization.

This work uses optimization study to formulate a patient-friendly antitussive fast-dissolving oral film based on phenylephrine hydrochloride (Phen) and dextromethorphan hydrobromide (Dex). The designed films were based on hydroxypropylmethyl cellulose (HPMC) with two grades (E5 and E50) as a film-forming polymer by the solvent-casting method. Polyethylene glycol with two molar masses (400 and 1000) was used as a plasticizer, while aspartame was used as a sweetener and microcrystalline cellulose intended to act as a disintegrant. To find an optimum formulation, a response surface methodology and a central composite design were employed. The percentage of HPMC E50, and PEG, as a plasticizer, were considered to be the design factors. Film thickness, surface pH, disintegration time, dissolution percent, tensile strength, elongation percent and folding endurance were considered to be the responses. A film with 11.46% E50, 88.54% E5, 25% of two drugs (8.4% of Phen and 16.6% of Dex) and 18.54% plasticizer is designed and prepared as the optimum formulation for Phen/Dex fast-dissolving oral films, with 95% confidence levels.

Formulation and evaluation of fast dissolving oral wafers of linagliptin

Wafers are modern oral dosage forms which are commonly used by patients worldwide. Also, in acute pain, these dosage types can be used to get immediate relief. These oral sublingual wafers are nothing more than a thin oral stripe which dissolves immediately due to the presence of saliva in the mouth when placed in the sublingual cavity by releasing medication within a short span of time. The faster dissolution can be achieved by using different superdisintegrants in different concentrations and a comparative study of different superdisintegrants has been carried out. Present investigation aims to formulate fast dissolving wafer of linagliptin using different film forming agents. From the latest research it can be inferred that fast-dissolving oral films of drug release are preferable. The films prepared by HPMC K4 and K15 and CCS and CP had shown strong mechanical power, release of narcotics, period for disintegration and analysis of dissolution. F7 formulation is considered the better with less disintegrating time and release in 10 min according to the results obtained. Percent drug release and disintegration time was taken as responses for study which were found within the accepted ranges.

Solubility Enhancement of Glipizide and Development of its Fast-dissolving Oral Film

Background: Difficulty in swallowing tablet dosage form is common among all ages people, especially old and pediatrics. Fast dissolving oral films (FDOFs) may represent an innovative dosage type that settles the issue of gulping and supply fast onset of action. Objective: The objective of the present investigation was to increase the solubility of poorly soluble Glipizide (BCS Class II) by solid dispersion technique and develop its FDOFs. Methods: A solvent evaporation process was used to make a solid dispersion of the Glipizide. The saturation solubility of glipizide and its solid dispersion was determined in a different solvent. For the film preparation, solvent casting method was chosen. The excipients were selected based on pre-formulation data. The composition of the film was optimized based on a trial-and-error basis using different concentrations of plasticizer. The average weight, thickness, disintegration time, tensile strength, surface pH, folding endurance, drug content, and in-vitro dissolution analysis of the films were all taken into consideration. Results: There was no incompatibility between drug / solid dispersion and the excipients. The solid dispersion of the glipizide showed improved solubility by almost 10 folds. Many of the formulated films disintegrated in less than 30 seconds. At the end of 5 minutes, the optimized film had released more than 90% of the compound. The prepared films were found to be stable at room temperature. Conclusion: The solubility of Glipizide was improved successfully by solubilization technique using soluplus. The FDOFs of the glipizide were successfully formulated using pullulan as polymer.

THE DEVELOPMENT AND CHARACTERISATION OF FAST DISSOLVING FILM OF POORLY WATERSOLUBLE DRUG LURASIDONE HYDROCHLORIDE

Objective: The objective of the present work was to formulate and evaluate a fast-dissolving oral film of lurasidone hydrochlorideused as an atypical antipsychotic for the treatment of schizophrenia capable of providing faster onset of action.
 Methods: The fastdissolving films of lurasidone hydrochloride were prepared by the solvent casting technique using different compositions and combinations of hydroxypropyl methylcellulose E-3, E-5, E-15, and K4M as fast-dissolving polymer bases. A set of seven formulations were prepared and evaluated for parameters like physical characterization, thickness, weight uniformity, mechanical characteristics (folding endurance,tensile strength), surface pH, in vitro disintegration time, drug content, and an in vitro drug release.
 Results: The prepared films exhibited uniform and a smooth surface with uniform weight, thicknessand 89-90% mg drug content. The formulation F7 Showed excellent elasticity and disintegration within seconds. Lurasidone hydrochloride was rapidly released in vitro from all formulations. The release was found to be rapid and maximum of 41.5% in Phosphate buffer pH 6.8 and 58.6% in 0.1 N hydrochloric acid over a period of 30 min. The further optimized formulation F7Adepicted a faster and maximum release of 78% as compared to the marketed tablet 74%.
 Conclusion: The developed formulation is a better alternative to tablets by its ability to produce good drug release.

Formulation of a fast-dissolving oral film using gelatin and sodium carboxymethyl cellulose

Background and objective: Orally disintegrating film is a solid dosage form made as an alternative for tablets for pediatric and geriatric patients who have difficulty in swallowing. These formulations are designed to dissolve in the mouth rapidly upon contact with saliva. This study aimed to prepare a thin oro-dispersible film base that can withstand handling in which a drug can be incorporated to provide a new dosage form. Methods: The solvent casting method was used to prepare the films, in which the ingredients were mixed, dissolved, and cast in a Petri dish. Then, they were left to dry in the oven overnight. Different concentrations of each of the two polymers alone and combined in different ratios were compared using different concentrations of plasticizer. Results: Successful, transparent films were prepared from gelatin and glycerin. A combination of 70% gelatin and 30% sodium carboxymethyl cellulose with glycerin formed an acceptable film having white color. The film forming capacity of sodium carboxymethyl cellulose alone was not good. All films were tearing and not well formed. All films that contain polyethylene glycol were brittle. Both superdisintegrants reduced the disintegration time for both films, but kyron was more effective than sodium starch glycolate. Conclusion: A successful oral film was prepared using different types of polymers, which is suitable for incorporating a potent drug to form a new dosage form that is easily portable and does not require water for swallowing. Keywords: Fast dissolving oral film; Gelatin; Sodium carboxy methyl cellulose; Solvent casting method.