Fast Dissolving Drug Delivery Systems Research Articles

Teneligliptin hydrobromide hydrate mouth dissolving strip: Formulation and evaluation

Oral route is considered as one of the most convenient route for administration of various pharmaceutical dosage form like tablet, capsule, syrup, suspension and emulsion. Fast Dissolving Drug Delivery systems have developed various fast disintegrating preparations like Oral disintegrating film, ODF. Oral disintegrating film is the solid oral drug delivery system, in which water soluble polymer involve to disintegrate film into mouth fastly. Oral disintegrating film is superior as compare to orally disintegrating tablet as the cost of production is low. The present research was undertaken to develop oral disintegrating film of tteneligliptin hydrobromide hydrate to have rapid onset of action. of tteneligliptin hydrobromide hydrate which is an anti-diabetic. The mechanism action of Teneligliptin is to increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels.The concept of formulating fast disintegrating film Teneligliptin containing offers a suitable and practical approach in serving desired objective of faster disintegration and dissolution characteristics with increased bioavailability. ODF of Teneligliptin were prepared by solvent casting method and evaluated physicochemical parameters like thickness, weight variation, moisture content, folding endurance, drug content, etc. All the formulations of Teneligliptin ODF displayed optimum folding endurance, which indicates the formulation prepared can withstand handling and transportation. From the results obtained, it was concluded that the formulation of oral disintegrating film has better physical chemical properties with good disintegration property.

A REVIEW ON MOUTH DISSOLVING FILM- A NOVEL APPROACH

The oral route is one of the most important routes for local and systemic drug delivery due to its large surface area, high permeability and blood flow. Mouth dissolving films are the most advanced oral forms as they are simpler and easier to use than other dosage forms such as Oro-soluble tablets, sublingual tablets. Fast dissolving drug delivery system were rapidly developed in the 1970s as an alternative to capsules, syrups, and tablets for adults and adolescents who have difficulty swallowing conventional oral solid dosage form. The Oro- soluble film dissolves and disintegrates in less than a minute when placed in the mouth without drinking water or chewing. This form allows the drug to skip first-pass metabolism, which improve the bioavailability of the drug. This article provides a comprehensive review on mechanism of action, merits, formulation, evaluation and covering the aspects related to novel fast dissolving techniques.

A REVIEW ON MOUTH DISSOLVING FILM

Oral route is considered as one of the most convenient route for administration of various pharmaceutical dosage forms like, tablet, capsule, syrup, suspension and emulsion. Fast Dissolving Drug Delivery systems have developed various fast disintegrating preparations like mouth dissolving film, MDT. Oral thin film are new dosage form that are prepared from hydrophilic polymer which are when placed in mouth, buccal cavity disintegrate rapidly. Mouth dissolving film is superior as compare to mouth dissolving tablet as the cost of production is low. Geriatric and pediatric patients are facing difficulty in swallowing of tablet and capsule, the oral film can bypass it, along with that it has other advantages like self-administrable, fast dissolving, rapid absorption that make it versatile dosage form. The aim of present study is to enlighten specifically different polymer along with their concentrations and applications. This study also focuses on use of plasticizer, polymer, sweetener, different methods which are used for the preparation of oral films and various evaluation parameter of the film.

Review On Fast Dissolving Drug Delivery System

Review On Fast Dissolving Drug Delivery System

Pre-formulation study of Bisoprolol as fast Dissolve Sublingual Tablet

Fast dissolving drug delivery systems offer a solution for patients having difficulty in swallowing tablets. In this study, an attempt had been made to perform pre-formulation studies of bisoprolol as fast dissolve sublingual tablet, an antihypertensive by direct compression methods using sodium-starch-glycolate, croscarmellose-sodium, & crospovidone as superdisintegrant agent. The basic purpose of the pre-formulation activity is to provide a basis for the formulation approaches, to maximize the chances of success in formulating an acceptable product, optimizing drug product quality and performance. Preformulating activity including drug melting point; analytical wavelength (λ max) detections, drug-excipients physical & chemical compatibility by FT-IR, and Calibration curve of Bisoprolol were studied. It was discovered that the melting point was 100°C, and the UV spectral analysis revealed that the maximum value of λ was between 224 and 273 nm. The physicochemical compatibility studies results indicate that there was no interaction between bisoprolol and the excipients. Strong linear relationship obtained from calibration curve. Based on results, fast dissolving sublingual tablets of Bisoprolol can be prepared successfully by direct compression.

Orally fast-dissolving drug delivery systems for pediatrics: Nanofibrous oral strips from isoniazid/cyclodextrin inclusion complexes

Isoniazid (INH) is an essential antibiotic for tuberculosis that suffers from low water-solubility and limited bioavailability due to its crystalline form. Generation of inclusion complex nanofibrous film of isoniazid with highly water soluble cyclodextrin derivates can enable to develop a new oral delivery system with fast-disintegrating feature. In this study, the inclusion complex (IC) of INH and hydroxypropyl-beta cyclodextrin (HPβCyD) were fabricated into nanofibrous film through electrospinning technique. Here, HPβCyD was used for both encapsulation of INH and electrospinning of free-standing nanofibrous films. Electrospinning of INH/HPβCyD-IC system resulted into uniform and homogenous fiber morphology having ∼400 nm mean diameter. The ultimate INH/HPβCyD-IC nanofibers were obtained with a ∼100% of loading efficiency (∼8% (w/w) of INH content) without loss of drug content during whole process. Due to inclusion complexation, the electrospinning and so the amorphization of INH within the INH/HPβCyD-IC nanofibrous film was achieved without the use of any organic solvents or toxic agents. The amorphous state of INH and the unique properties of nanofibrous matrix ensured faster and enhanced release profile for INH molecules compared to its pristine powder form. Additionally, INH/HPβCyD-IC nanofibrous film presented a quite fast-disintegration profile in the saliva simulation (∼2s). Overall, this approach revealed a promising administration way as orally fast-dissolving drug delivery system especially for pediatric patients.

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

Assessment of Lornoxicam as a Mouth Dissolving film in Management of Post Extraction Pain-A Randomized Control Trial

Background: Mouth dissolving film (MDF) is a fast-dissolving drug delivery system that provides a practical means to administer drugs not just to special populations with swallowing difficulties but also to the general public. MDFs are novel dosage forms that dissolve and disintegrate quickly within the mouth. Aim: To assess the efficacy of lornoxicam mouth dissolving film as a potent analgesic and drug delivery system and compare it with the aceclofenac tablet in the management of post-extraction pain. Methodology: The study group comprised 60 subjects of either sex of age group 20–50 years who were divided into an experimental group (group A) and a control group (group B). Group A was administered lornoxicam MDF and group B was administered aceclofenac tablets. Pre-treatment and post-treatment pain assessments were recorded using a visual analog scale (VAS) and an oral pain scale (OPS). Results: In a comparison of the mean value of pre-treatment VAS and VAS after 24 h, the percentage of pain reduction in group A was 86.66%, and in group B was 75%. When comparing the mean value of pre-treatment OPS and OPS after 24 h, the percentage of pain reduction in group A was 93.33% and in group B was 75%. These results were statistically significant, with a P value of 0.00 in both groups. Conclusion: Lornoxicam as an MDF showed promising results in managing post-extraction pain. The potential delivery of lornoxicam through the MDF was safe, with better patient compliance, and no reported cases of adverse effects.

Fast Dissolving Tablets: A Review

In the pharmaceutical Industry oral route is considered as the safest and convenient route. Fast dissolving tablets (FDTs) are solid dosage forms containing drugs that disintegrate in the oral cavity within less than 1 minute leaving an easy to swallow residue. These dosage forms include superdisintegrants which impart quick disintegration with existence of saliva and can be swallowed without difficulty. Fast dissolving tablets are the very good preference for the paediatric as well as geriatric patients. To improve the bioavailability of many drugs, fast dissolving drug delivery systems are used widely. Sophisticated technologies used for manufacturing fast dissolving tablets are by direct compression method, freeze drying method, sublimation method, mass extrusion and cotton candy process. Taste is the vital factor since these tablets disintegrate directly in the mouth. FDTs are evaluated by various parameters such as hardness test, friability test, water absorption ratio, wetting time, disintegration test and dissolution test. These tablets are also well-known as mouth dissolving tablets and orodispersible tablets. This review article will emphasize on ideal properties, challenges, advantages, disadvantages, conventional techniques, patented technologies and evaluation of orodispersible tablets.

Research the influence of excipients on the technological properties of captopril fast dissolving films

Drug-loaded films are of great interest among fast-dissolving drug-delivery systems. The creation of fast-dissolving films for the treatment of cardiovascular diseases is important.The first inhibitor of angiotensin-converting enzyme to appear on the world market was captopril, which is used to treat hypertension, chronic heart failure and others. Captopril has an antihypertensive effect, which manifests itself within 5–15 minutes after sublingual administration.
 The aim of our study was to develop the technology of captopril fast dissolving films by solvent casting method and analyze the influence of groups of excipients on technological properties of the films.
 The influence of the character of polymers, plasticizers, disintegrants and sweeteners on the technological properties of experimental batches of captopril fast dissolving films was studied. Such technological indicators as uniformity of weight, thickness, swelling index,tensile strength, elongationand disintegration time were studied.
 The influence of excipients' composition on the technological indicators of captopril fast dissolving films has been researched. It was found out that the effect of the type of polymer had the decisive influence on all parameters of films.The selected plasticizer determined the elasticity (films' elongation), film thickness and weight variation. Optimal values of the average weight and thickness of captopril films are provided by the use of a polymer in the combination of HPMC with PEG 4000 or a combination of HPMC with PEG 6000, as a plasticizer – glycerin or PEG 400. The best results of films' swelling were obtained with the introduction of HPMC brands Metolose® 90 SH 100 000 or Metolose® 65 SH 50, Polyplasdone XL-10 crospovidone, propylene glycol and sorbitol. The disintegration time less than 3 min was observed in all investigated film compositions, except those containing PVA. The highest value of tensile strength for captopril films was obtained using HPMC brand Metolose® 65 SH 50 or Metolose®90 SH 100 000.
 Using the desirability function, the optimal excipients within the studied groups were selected.It has been established that the optimal values of the technological parameters of captopril films can be achieved using Hydroxypropyl MethylcelluloseVivapharm® E15, polyethylene glycol 400, sodium starch glycolate and sorbitol.

Oral Thin-films from Design to Delivery: A Pharmaceutical Viewpoint

Stable drug-type tablets and capsules are painful to drink or chew for many pediatric and geriatric patients. Accurate dosing is also an issue for liquid orals (syrup, suspension, emulsion, and so on). Several fast-dissolving drug delivery systems have been designed to address these issues. One of the innovative methods for rapid drug delivery with self-administration without water or chewing is a thin polymer oral drug strip. Strip-forming polymers, plasticizers, active pharmaceutical ingredients, sweetening agents, saliva enhancing agents, flavoring agents, coloring agents, stabilizing and thickening agents are all used to form oral drug strips. The scope of oral thin films is expanded in this article.

A Short Review on “A Novel Approach in Fast Dissolving Film & their Evaluation Studies”

In the case of chronic illnesses, fast-dissolving drug delivery systems were developed as an oral medication administration alternative to traditional dose forms. For masking the taste of unpleasant drugs and enhancing patient compliance, fast-dissolving films are now recommended over traditional tablets and capsules. Fast dissolving films consist of a very thin oral strip that dissolves in less than one minute when placed on the tongue. Customers have responded positively to dissolvable oral thin films in the form of breath strips, which have been on the market for a few years and are used to administer vitamins, vaccines and other medicinal products. In fact, the review goes through the various production methods for film preparation. The current review summarizes the majority of recent patents on fast-dissolving films. A brief analysis of the several factors considered to analyze such films has been carried out. These fast-dissolving films are better to other oral traditional dose forms in terms of delivering drugs and attaining faster therapeutic blood levels in the case of chronic diseases.

An overview on FDA-approved natural super disintegrants efficacy in a fast dissolving drug delivery system

FDTs are defined by the United States Food and Drug Administration (FDA) as a solid dosage form containing the therapeutic substance or when applied on the tongue, the active ingredient disintegrates quickly, usually within seconds. The goal of this study is to create a fast-dissolving tablet that uses natural disintegrants. Fast dissolving tablets have grown in popularity in the pharmaceutical industry in recent years. They have a quick disintegration activity that dissolves with saliva without the use of water when placed within the mouth. Furthermore, FDT aims to provide quick medication absorption, reduced toxicity, and higher drug bioavailability, and it is especially popular among geriatric and paediatric patients. Natural disintegrants, which are obtained from natural sources, have a number of advantages, including low cost, nontoxicity, biodegradability, environmental friendliness, and less adverse effects. As a result, it has been established that natural disintegrants are often safer than synthetic disintegrants. Natural disintegrants includes Chitin and chitosan, Guar gum, Gum karaya, Agar and treated agar, Fenugreek seed mucilage, Soy polysaccharide, Gellan gum, Mango peel pectin, Lepidium sativum mucilage, Plantago seed mucilage, Agele marmelos gum, Locust bean gum, Mangifera indica gum, Hibiscus rosa sinensis mucilage, Dehydrated banana powder.

A Review on Fast Dissolving Oral Films

Oral route are the most convenient and common route of administration of drug because of the low cost of therapy and ease of administration lead to high levels of patient compliance as in the form of tablets and capsules. Generally In some cases, the oral solid dosage form may become difficult especially in swallowing. So to overcome these problems, fast dissolving drug delivery systems have been developed which disintegrate or dissolve within one minute when placed in the mouth without water or chewing. These are the formulations administered without water. These thin sized oral film stripes are designed in such a manner for the ease administration of drug when film is placed on or under the tongue. These film enables the drug to deliver directly in to the blood stream either through buccal or sublingually. Oral films improve the onset of action, lower the dosing and enhance the bioavailability.

Development of Nanonized Nitrendipine and Its Transformation into Nanoparticulate Oral Fast Dissolving Drug Delivery System.

The present research focuses on the development of a nanoparticulate (nanocrystals-loaded) rapidly dissolving (orodispersible) tablet with improved solubility and bioavailability. The nanosuspension (NS) was prepared by antisolvent sonoprecipitation technique and the optimized NS was lyophilized to obtain nanocrystals (NCs), which were evaluated for various parameters. The nitrendipine (NIT) nanoparticulate orodispersible tablet (N-ODT) was prepared by direct compression method. The optimized N-ODT was evaluated for pre and post compression characteristics, in vivo pharmacokinetic and stability profile. The optimized NS showed a particle size of 505.74 ± 15.48 nm with a polydispersity index (PDI) of 0.083 ± 0.006. The % NIT content in the NCs was found to be 78.4 ± 2.3%. The saturation solubility of NIT was increased remarkably (26.14 times) in comparison to plain NIT, post NCs development. The DSC and p-XRD analysis of NCs revealed the perseverance of the integrity and crystallinity of NIT on lyophilization. The results of micromeritic studies revealed the good flow-ability and compressibility of NCs blend. All the post-compression properties of N-ODT were observed within the standard intended limit. The dispersion, wetting, and disintegration time of the optimized batch of N-ODT was found to be 39 ± 1.13 s, 44.66 ± 1.52 s, and 33.91 ± 0.94 s respectively. The in vitro dissolution study displayed 100.28 ± 2.64% and 100.61 ± 3.3% of NIT released from NCs (in 8 min) and N-ODT (in 6 min) respectively, while conventional NIT tablet took 30 min to release 99.94 ± 1.57% of NIT. The in vivo pharmacokinetic study in rabbits demonstrated significantly (p < 0.05) higher bioavailability of NIT on release from N-ODT than the conventional NIT tablet. Thus, N-ODT could be a promising tool for improving the solubility and bioavailability of NIT and to treat cardiovascular diseases effectively.

Formulation, Optimization and Evaluation of Nanofiber Based Fast Dissolving Drug Delivery System of Colchicine for Pediatrics

Systemic toxicity is an obstacle against the oral administration of colchicine. The high body surface area to mass ratio in pediatrics would dramatically enhance the toxicity risk. This issue could be jettisoned by formulation of an optimized nanofiber-based fast dissolving delivery system. It could enhance the drug's bioavailability, reduce the administered dose, and bring more convenience and compliance for pediatrics with the problem of consuming conventional dosage forms. The optimized colchicine loaded nanofibers of polyvinyl alcohol 10%w/v with 220.47±16.87 nm mean diameter size exhibits smooth surface and continuous structure in SEM micrographs. No incompatibility was seen in FT-IR analyses. The thermal study illustrated stability enhancement by colchicine loading. The water angle analysis demonstrated its superhydrophilicity and the in vitro release profile illustrated a quick release of colchicine in 30 seconds. As a conclusion, nanofiber-based fast dissolving formulation of colchicine could be suggested as a localized and systemic transmucosal delivery system, immediate-release oral dosage form, and even topical colchicine delivery system that may reduce the risk of systemic toxicity in pediatrics. The antitumor property of CL may also suggest it in rapid neoadjuvant or adjuvant localized chemotherapy protocols for the management of topical tumors in pediatrics.

Fast Dissolution Electrospun Medicated Nanofibers for Effective Delivery of Poorly Water-Soluble Drug.

Electrospinning is developing rapidly from an earlier laboratory method into an industrial process. The clinical applications of this technique are approached in various ways through electrospun medicated nanofibers. Fast-dissolving oral drug delivery systems (DDSs) have promising commercial applications in the near future. Related papers have been investigated in this study, including the latest research results on electrospun nanofiber-based fast-dissolution DDSs. The following related topics are concluded: 1) development of electrospinning, ranging from one-fluid blending to multi-fluid process and potential applications in the formation of medicated nanofibers involving poorly water-soluble drugs; 2) selection of appropriate polymer matrices and drug carriers for filament formation; 3) types of poorly water-soluble drugs ideal for fast oral delivery; 4) methods for evaluating fast-dissolving nanofibers; 5) mechanisms that promote the fast dissolution of poorly water-soluble drugs by electrospun nanofibers; 6) and important issues related to further development of electrospun medicated nanofibers as oral fast-dissolving drug delivery systems. Given their unique properties, electrospun-medicated nanofibers can be used as oral fast-dissolving DDSs of poorly water-soluble drugs. However, significant issues, such as scalable productions and solid dosage form conversions, need to be investigated.

Fast Dissolving Electrospun Nanofibers Fabricated from Jelly Fig Polysaccharide/Pullulan for Drug Delivery Applications.

The fast-dissolving drug delivery systems (FDDDSs) are developed as nanofibers using food-grade water-soluble hydrophilic biopolymers that can disintegrate fast in the oral cavity and deliver drugs. Jelly fig polysaccharide (JFP) and pullulan were blended to prepare fast-dissolving nanofiber by electrospinning. The continuous and uniform nanofibers were produced from the solution of 1% (w/w) JFP, 12% (w/w) pullulan, and 1 wt% Triton X-305. The SEM images confirmed that the prepared nanofibers exhibited uniform morphology with an average diameter of 144 ± 19 nm. The inclusion of JFP in pullulan was confirmed by TGA and FTIR studies. XRD analysis revealed that the increased crystallinity of JFP/pullulan nanofiber was observed due to the formation of intermolecular hydrogen bonds. The tensile strength and water vapor permeability of the JFP/pullulan nanofiber membrane were also enhanced considerably compared to pullulan nanofiber. The JFP/pullulan nanofibers loaded with hydrophobic model drugs like ampicillin and dexamethasone were rapidly dissolved in water within 60 s and release the encapsulants dispersive into the surrounding. The antibacterial activity, fast disintegration properties of the JFP/pullulan nanofiber were also confirmed by the zone of inhibition and UV spectrum studies. Hence, JFP/pullulan nanofibers could be a promising carrier to encapsulate hydrophobic drugs for fast-dissolving/disintegrating delivery applications.

Developing and scaling up fast-dissolving electrospun formulations based on poly(vinylpyrrolidone) and ketoprofen

Poly(vinyl pyrrolidone) (PVP) electrospun fibers loaded with ketoprofen were fabricated in this work as potential fast dissolving drug delivery systems (DDSs) for oral delivery. By changing the processing parameters and collector geometry it was possible to increase the throughput rate from 1 to 20 mL/h. The fibers all took the shape of cylinders and had smooth surfaces. They comprise amorphous solid dispersions of drug-in-polymer, with very high drug encapsulation efficiencies (100%). With a low drug loading (9.09% w/w) the electrospun materials could disintegrate quickly and accelerate the dissolution profile of ketoprofen under non-sink conditions representative of the oral cavity. However, at higher loadings (23.08% w/w), this benefit is no longer realized, indicating that there is a maximum drug loading above which the dissolution-enhancing properties of the amorphous form and the hydrophilic PVP carrier cease to be effective. After storage under ambient conditions (19–21 °C, relative humidity 30–40%) for 4 weeks, the formulations remained amorphous, with no significant changes in their drug release properties. Very similar behaviour in terms of drug release and storage stability was seen regardless of the throughput rate used for fiber fabrication, showing the potential to rapidly produce large amounts of high-performing material.

Rospective designing and types of buccal drug delivery system: The Review

Buccal bioadhesive films, releasing topical drugs in the oral cavity at a slow and predetermined rate, provide distinct advantages over traditional dosage forms for treatment of many diseases. The mucosa of the buccal cavity is the most easily accessible transmucosal site. This fast dissolving drug delivery system (FDDS) is suited for the drugs which undergo high first pass metabolism and is used for improving bioavailability with reducing dosing frequency to mouth plasma peak levels, which in turn minimize adverse/side effects and also make it cost effective This article aims to review the recent Designs of buccal patches and their developments in the buccal adhesive drug delivery systems, & Buccal drug delivery is a promising area for continued research with the aim of systemic delivery of orally inefficient drugs as well as a feasible and attractive alternative for non-invasive delivery of potent peptide and protein drug molecules.