Modified Drug Release Research Articles

Preparation and Characterization of Pitavastatin Calcium Loaded Biodegradable Porous Starch as Carrier Platform for Drug Delivery

Introduction: Poor solubility and low oral bioavailability are major obstacles to the development of efficient drug delivery approaches. Numerous chemical entities fall into the biopharmaceutics classification system II (BCS II) class, categorized by low solubility and high permeability. Consequently, finding alternative solutions for improving drug efficacy becomes crucial. Hence, this study aims to formulate biodegradable porous acetostarch (BPSa) and biodegradable porous ethostarch (BPSe) carriers to augment the solubility profile of the poorly soluble drug candidate pitavastatin calcium (PTC). Method: The biodegradable carriers (BPSa and BPSe) were prepared using the solvent exchange method. Then the PTC was loaded into the prepared carriers (PTC@BPSa and PTC@BPSe) using the passive drug loading procedure. Moreover, the obtained drug-carrier conjugates were evaluated using physiochemical evaluation techniques such as Fourier transform infrared spectroscopy (FTIR), x-ray powder diffraction (XRPD), and differential scanning calorimetry (DSC). Additionally, the surface morphology and drug release characteristics are determined. Result: The experimental findings exhibited high drug content with 75.45% and 71.81% for PTC@BPSa and PTC@BPSe, respectively. The SEM analysis of the prepared conjugates demonstrates asymmetrical morphology with cracks between particles, indicating porous nature of the carriers. As a result of this, PTC@BPSa and PTC@BPSe exhibited modified drug release patterns, with cumulative releases of 78.63% and 78.50%, respectively. Conclusion: The biodegradable porous carriers (BPSa and BPSe) effectively improve the dissolution pattern of PTC, by addressing the challenges associated with poor solubility. This study offers valuable insights into the potential of these biodegradable porous carriers as effective drug delivery platforms for increasing the efficacy of limited soluble medications.

Synthesis and Characterization of Polymer-Based Membranes for Methotrexate Drug Delivery.

Methotrexate or amethopterin or 4-amino-N10-methyl pteroylglutamic acid is used for treating autoimmune diseases, as well as certain malignancies. Drug delivery systems, which are based on biopolymers, can be developed to improve the therapeutic and pharmacological properties of topically administered drugs. Biopolymers improve the therapeutic effect of drugs, mainly by improving their biodistribution and modulating drug release. This study presents the synthesis of membranes based on anionic polysaccharides and cationic polysaccharides for transdermal delivery of the active ingredient methotrexate, as well as a compatibility study between methotrexate and each of the components used in the prepared membranes. The obtained membranes based on different marine polysaccharides, namely κ-carrageenan and chitosan, for the release of the active ingredient methotrexate were characterized using techniques such as TG, FTIR, UV-Vis spectrophotometry, FTIR microscopy, water absorption capacity, water vapor permeability, and biodegradation rate. Following the studies, the membranes suitable for the transdermal release of the active substance were validated.

A dual pH- and temperature-responsive hydrogel produced in situ crosslinking of cyclodextrin-cellulose for wound healing

Cellulose hydrogels have gained attention in the field of wound healing due to their biodegradability, biocompatibility, and the capacity to sustain a humid environment that promotes healing. Conventional cellulose hydrogels were usually lacked responsiveness to changing wound conditions, and limited capacity for controlled release of active substances. The composite hydrogels with Berberine (BBR) loading were prepared from bamboo parenchymal cellulose and in situ crosslinking carboxylated-β-cyclodextrin (BPCH-B) via dissolution. The inclusion of BBR enhanced the antibacterial properties of cellulose hydrogel while maintaining biocompatibility and drug delivery capabilities. The dual-responsive dressing was demonstrated to modulate drug release kinetics in accordance with the pH and temperature conditions prevailing within the wound site. Specifically, study exhibited a significant increase in drug release (over 70 %) under alkaline pH (7.6) and temperature (40 °C) conditions. Full-thickness wound healing experiments indicated that BPCH-B had better healing ability, and the wound healing area of BPCH-B treated was 80 % within 12 days, while the control group was only 50 %. This strategy for generating functional wound healing can be further control release of drug compounds for treatment of wounds, enabling development of practical wound care materials.

Resveratrol-Laden Nano-Systems in the Cancer Environment: Views and Reviews.

The genesis of cancer is a precisely organized process in which normal cells undergo genetic alterations that cause the cells to multiply abnormally, colonize, and metastasize to other organs such as the liver, lungs, colon, and brain. Potential drugs that could modify these carcinogenic pathways are the ones that will be used in clinical trials as anti-cancer drugs. Resveratrol (RES) is a polyphenolic natural antitoxin that has been utilized for the treatment of several diseases, owing to its ability to scavenge free radicals, control the expression and activity of antioxidant enzymes, and have effects on inflammation, cancer, aging, diabetes, and cardioprotection. Although RES has a variety of pharmacological uses and shows promising applications in natural medicine, its unpredictable pharmacokinetics compromise its therapeutic efficacy and prevent its use in clinical settings. RES has been encapsulated into various nanocarriers, such as liposomes, polymeric nanoparticles, lipidic nanocarriers, and inorganic nanoparticles, to address these issues. These nanocarriers can modulate drug release, increase bioavailability, and reach therapeutically relevant plasma concentrations. Studies on resveratrol-rich nano-formulations in various cancer types are compiled in the current article. Studies relating to enhanced drug stability, increased therapeutic potential in terms of pharmacokinetics and pharmacodynamics, and reduced toxicity to cells and tissues are the main topics of this research. To keep the readers informed about the current state of resveratrol nano-formulations from an industrial perspective, some recent and significant patent literature has also been provided. Here, the prospects for nano-formulations are briefly discussed, along with machine learning and pharmacometrics methods for resolving resveratrol's pharmacokinetic concerns.

Microsponge: An Advanced Drug Delivery System

Abstract: Porous microsponges are a type of polymeric delivery method. These tiny, spherical particles, resembling sponges, have a large porous surface, which helps to modify drug release, stabilize the substance, and lessen side effects. To keep dose forms on the skin, micro sponges can be successfully included intopical medicine administration systems. Since the outer surface is frequently porous, the material can continuously flow out of the sphere. This system can suspend or entrap a variety of substances, and it can be incorporated into a manufactured product like a liquid, gel, cream, or powder. The majority of vehicles and components can be used with these formulations, which are stable in the pH range of 1 to 11 and up to 130ºC. Microsponges are created to reduce side effects, change medication release, and enhance stability to successfully distribute a pharmaceutically active component at the lowest amount achievable.

FORMULATION AND EVALUATION OF MOUTH DISSOLVING FILM OF CARIPRAZINE HYDROCHLORIDE

Mouth dissolving film is now a days preferred route of drug administration due to patient compliance. The developed film formulation is a patient-friendly formulation that would be useful for people who have difficulty of swallowing. The results have shown that the HPMC-K4M is good film former and shows bioadhesion property. In combination with PEG-400, it has shown promising fast drug release within 10 min. and good folding endurance. Hence a semi-synthetic cellulose derivative which is affordable and abundantly available can be used as a potential drug release modifier and also used to improve flexibility and processability in the mouth dissolving films. Successful formulation of Cariprazine mouth dissolving films may prevent first pass metabolism to a large possible extent. From the present study it can be concluded that HPMC-K4M based mouth dissolving films of Cariprazine can be successfully prepared with considerable good stability and improved bioavailability Keywords: Mpouth dissolving, Cariprazine, Evaluation

Gelatinized tapioca starch−magnesium aluminum silicate nanocomposites: Physicochemical characterization and evaluation for modified-release tablets

The objectives of this work were to prepare and investigate gelatinized tapioca starch-magnesium aluminum silicate (GTS-MAS) composites for use in modified-release tablets. The dispersions consisting of GTS and MAS with various ratios and %solid content were prepared and dried by spray drying to get the GTS-MAS composites. GTS could molecularly interact with MAS via hydrogen bonding, leading to an enhancement of thixotropic properties in the dispersion and the formation of exfoliated nanocomposites after drying. The GTS-MAS composites presented an elliptical shape with wrinkle shrinkage, powder bulkiness, and poor particle flowability. However, they had better particle flowability and tablet compressibility than the GTS particles. The drug-loaded GTS-MAS tablets provided remarkably higher hardness than the drug-loaded GTS tablets. The shorter disintegration time and the faster drug release of the tablets were found when increasing MAS ratios because the composites with higher MAS ratios displayed higher swelling capacity in both acidic and neutral media. Thus, drug diffusion coupled with swelling/erosion of the gel matrix could retard drug release from tablets. These findings suggested that the GTS-MAS nanocomposites could be employed as a matrix former in tablets intended for modifying drug release.

PREPARATION OF CRYSTALLINITY TAILORED SILK FIBROIN-SODIUM ALGINATE BASED FLOATING MICROBEADS FOR NEVIRAPINE DELIVERY

The present work anticipated crystallinity-tuned silk fibroin (SFIB)-sodium alginate floating microbeads (MB) as a candidate for nevirapine (NEV) sustained release. Briefly, crystallinity tuning was accomplished using solvent annealing. The changes in structural conformation of SFIB were validated using FTIR spectroscopy. Here, the tangent baseline method revealed changes in crystallinity of floating NEV-loaded SFIB-MB. Importantly, solvent annealing offers conversion of amorphous ‘α-helix’ to crystalline ‘β-sheet’ of SFIB, helping to modify drug release from the matrix of SFIB-sodium alginate. As well, NEV-loaded SFIB-MB demonstrated good floating profile. The NEV-loaded SFIB-MB with ethanol (ETH-6) annealing for 6 hours shows 25.853% drug release at 12 hours (pH = 1.2), compared to untreated NEV-loaded SFIB-MB (65.132%, 12 hours, log p < 0.0001). The release kinetics of batch ETH-6 revealed first-order release kinetics and Fickian diffusion (n = 0.468) was found to be the drug diffusion mechanism. Therefore, crystallinity-modified floating NEV-loaded SFIB-based MB will open a new door for modified drug delivery.

Magnetic-Responsive Liposomal Hydrogel Membranes for Controlled Release of Small Bioactive Molecules-An Insight into the Release Kinetics.

This work explores the unique features of magnetic-responsive hydrogels to obtain liposomal hydrogel delivery platforms capable of precise magnetically modulated drug release based on the mechanical responses of these hydrogels when exposed to an external magnetic field. Magnetic-responsive liposomal hydrogel delivery systems were prepared by encapsulation of 1,2-dipalmitoyl-sn-glycero-3-phosphocoline (DPPC) multilayered vesicles (MLVs) loaded with ferulic acid (FA), i.e., DPPC:FA liposomes, into gelatin hydrogel membranes containing dispersed iron oxide nanoparticles (MNPs), i.e., magnetic-responsive gelatin. The FA release mechanisms and kinetics from magnetic-responsive liposomal gelatin were studied and compared with those obtained with conventional drug delivery systems, e.g., free liposomal suspensions and hydrogel matrices, to access the effect of liposome entrapment and magnetic field on FA delivery. FA release from liposomal gelatin membranes was well described by the Korsmeyer-Peppas model, indicating that FA release occurred under a controlled diffusional regime, with or without magnetic stimulation. DPPC:FA liposomal gelatin systems provided smoother controlled FA release, relative to that obtained with the liposome suspensions and with the hydrogel platforms, suggesting the promising application of liposomal hydrogel systems in longer-term therapeutics. The magnetic field, with low intensity (0.08 T), was found to stimulate the FA release from magnetic-responsive liposomal gelatin systems, increasing the release rates while shifting the FA release to a quasi-Fickian mechanism. The magnetic-responsive liposomal hydrogels developed in this work offer the possibility to magnetically activate drug release from these liposomal platforms based on a non-thermal related delivery strategy, paving the way for the development of novel and more efficient applications of MLVs and liposomal delivery systems in biomedicine.

The Impact of Hypromellose on Pharmaceutical Properties of Alginate Microparticles as Novel Drug Carriers for Posaconazole.

Fungal infections are a group of diseases which are challenging to treat because of drug-resistant fungi species, drug toxicity, and often severe patient conditions. Hence, research into new treatments, including new therapeutic substances and novel drug delivery systems, is being performed. Mucoadhesive dosage forms are beneficial to improving drug bioavailability by prolonging the residence time at the site of application. Sodium alginate is a natural polymer with favorable mucoadhesive and gelling properties, although its precipitation in acidic pH significantly disrupts the process of drug release in gastric conditions. Hypromellose is a hydrophilic, semi-synthetic cellulose derivative with mucoadhesive properties, which is widely used as a control release agent in pharmaceutical technology. The aim of this study was to evaluate the impact of hypromellose on alginate microparticles with posaconazole, designed to modify drug release and to improve their mucoadhesive properties for both oral or vaginal application.

Gastroretentive Drug Delivery System in Cancer Chemotherapy.

Chemotherapy for stomach cancer often includes several side effects. The primary reasons for the failure of such treatment approaches are low drug concentrations in target tissues and a short stomach residence time. Gastroretentive controlled drug delivery systems improves the therapeutic performance of chemotherapeutic drugs following oral administration because of the longer gastric retention time. The goal of this study was to find suitable gastroretentive formulations that might be used for the localized treatment of stomach cancer. The purpose of this study is to summarize current advances in gastro-retentive drug administration for oral chemotherapy, with a focus on floating, mucoadhesive, and swellable systems. This article also discusses the potentials and limitations of existing gastroretentive drug delivery systems used in cancer chemotherapy. Due to increased stomach retention and modified drug release properties, gastroretentive controlled drug delivery systems improve the therapeutic performance of anti-cancer drugs used to treat stomach cancer. Gastroretentive drug delivery systems appear to be a promising carrier for localized chemotherapy with smaller doses and better patient compliance. However, selection of drug candidates, drugfood interactions and chemotherapy-induced gastric discomfort remain the key characteristics that must be addressed to improve treatment outcomes.

Modifying Drug Release for Intramuscular and Oral Delivery Using Drug-eluting Embolisation Beads

In recent years, polymer-based embolisation beads have been used to deliver drugs for the treatment of cancer directly to the site of action. Known to be biocompatible implants, these beads have become an ideal drug delivery vehicle for parenteral administration yet have not been considered for the more commonly used drug delivery routes such as oral and intramuscular drug delivery. This work describes the application of a type of polymer beads, formerly used for embolisation, as a formulation option for oral and intramuscular delivery of a model drug, namely imipramine. Following successful incorporation within the beads, dissolution analysis confirmed the potential to provide a modified drug release profile. Thermogravimetric analysis (TGA) permitted determination of the total water content within the beads (96.8%) and differential scanning calorimetry (DSC) indicated that not all of the water within the beads was able to freeze, apportioned as 15.8% non-freezing, 25.1% loosely bound and the remaining 55.9% unbound. In the presence of drug, the size of the beads decreased with a reduced water content (95.4%) comprised of 16.7% non-freezing, 20.5% freezing bound and the remaining 58.2% % unbound.In conclusion, the results presented in this study confirm the ability of TGA and DSC to separate the differing types of water within the beads and furthermore, the potential of such beads for a far wider variety of formulation options than those previously adopted.

Layer by layer self-assembly for coating a nanosuspension to modify drug release and stability for oral delivery

Layer-by-layer (LbL) modification is an effective way to tune the properties of particles. However, the traditional LbL process involves repeated washing steps which are not compatible with nanoparticles with a partial solubility. In this work, we demonstrate the use of a titration method for producing LbL coatings onto a nanosuspension of curcumin (a compound with a limited aqueous solubility). The aim of the work was to show how LbL can be used to enhance the release behaviour and stability of the curcumin in a nanosuspension form. Coated nanosuspension samples were produced using biocompatible and biodegradable polyelectrolytes, poly-l-arginine, and sodium alginate and was sizes approximately 500 nm. A stimuli-responsive nanosuspension was prepared by coating the nanosuspension with 5 layers of poly-l-arginine and alginate and Eudragit L100 as an outmost layer. The in vitro release of these nanosuspensions revealed that the use of a pH-responsive layer (Eudragit L100) as an outermost shell resulted in delay the release of curcumin (5%) in acidic pH and facilities its release in neutral pH (11%) over 72 h. Additionally, the bioaccessibility study showed that increasing the number of layers resulted in increasing the stability curcumin in nanosuspension when exposed to conditions that mimic the gastrointestinal tract from 20% for uncoated nanosuspension to 40% and 90% for 4-layered coated nanosuspension and stimuli-responsive (6-layered) coated nanosuspension, respectively. The cytotoxicity of LbL-coating of nanosuspension revealed a reduction in the toxicity of curcumin. This work shows how a titrated LbL modification approach could be used to tailor the stability and the release behaviour of nanosuspensions for oral drug delivery applications.

Size-dependence of the skin penetration of andrographolide nanosuspensions: In vitro release-ex vivo permeation correlation and visualization of the delivery pathway

Particle size is a key parameter to determine the capacity of nanoparticles to overcome the skin barrier; however, such effect and the possible mechanism remain only partially understood for nanosuspensions. In this work, we examined the skin delivery performance of andrographolide nanosuspensions (AG-NS) ranging in diameter from 250 nm to 1000 nm and analyzed the role of particle size in influencing their ability of skin penetration. The AG-NS with particle sizes of about 250 nm (AG-NS250), 450 nm (AG-NS450), and 1000 nm (AG-NS1000) were successfully prepared by ultrasonic dispersion method and characterized by transmission electron microscopy. The drug release and penetration via the intact and barrier-removed skin were compared by the Franz cell method, and the related mechanisms were probed using laser scanning confocal microscopy (LSCM) via visualization of penetration routes and histopathological study via observation of structural change of the skin. Our finding revealed that drug retention in the skin or its sub-layers was increased with the reduction of particle size, and the drug permeability through the skin also exhibited an obvious dependence on the particle size from 250 nm to 1000 nm. The linear relationship between the in vitro drug release and ex vivo permeation through the intact skin was well established among different preparations and in each preparation, indicating the skin permeation of the drug was mainly determined by the release process. The LSCM indicated that all these nanosuspensions could deliver the drug into the intercellular lipid space, as well as block the hair follicle in the skin, where a similar size dependence was also observed. The histopathological investigation showed that the formulations could make the stratum corneum of the skin loose and swelling without severe irritation. In conclusion, the reduction of particle size of nanosuspension would facilitate topical drug retention mainly via the modulation of drug release.

Carrageenan/Chitin Nanowhiskers Cryogels for Vaginal Delivery of Metronidazole.

The development of polymeric carriers based on partially deacetylated chitin nanowhiskers (CNWs) and anionic sulfated polysaccharides is an attractive strategy for improved vaginal delivery with modified drug release profiles. This study focuses on the development of metronidazole (MET)-containing cryogels based on carrageenan (CRG) and CNWs. The desired cryogels were obtained by electrostatic interactions between the amino groups of CNWs and the sulfate groups of CRG and by the formation of additional hydrogen bonds, as well as by entanglement of carrageenan macrochains. It was shown that the introduction of 5% CNWs significantly increased the strength of the initial hydrogel and ensured the formation of a homogeneous cryogel structure, resulting in sustained MET release within 24 h. At the same time, when the CNW content was increased to 10%, the system collapsed with the formation of discrete cryogels, demonstrating MET release within 12 h. The mechanism of prolonged drug release was mediated by polymer swelling and chain relaxation in the polymer matrix and correlated well with the Korsmeyer-Peppas and Peppas-Sahlin models. In vitro tests showed that the developed cryogels had a prolonged (24 h) antiprotozoal effect against Trichomonas, including MET-resistant strains. Thus, the new cryogels with MET may be promising dosage forms for the treatment of vaginal infections.

A REVIEW ON THE SOLID ORAL DOSAGE FORM FOR PEDIATRICS, REGULATORY ASPECTS, CHALLENGES INVOLVED DURING THE FORMULATION, AND TOXICITY OF THE EXCIPIENTS USED IN PEDIATRIC FORMULATION

Designing an appropriate dosage form in medical treatment for the pediatric population is very challenging. The major challenges faced during designing the oral solid dosage form for pediatrics are also the prerequisites for the development of the dosage form, and they are, administering the drug according to the body weight and taste masking, which is followed by other factors like the safety of excipients, size of dosage form and so on. Oral solid dosage forms like mini-tablets, soluble films, and orally disintegrating tablets are a few promising dosage forms for use in the pediatric population. The obstacles, such as physiological differences between the various age groups, excipient safety, technology requirements, low profitability, clinical trial limitations, and regulatory ambiguity all have an impact on pediatric dosage form development. Recent advancement in the development of pediatrics formulations has been made due to new regulations, more financial opportunities, and novel collaborative research programs. A shift of pattern towards solid oral dosage form and an emphasis on innovative preparations, such as dispersible, flexible, as well as multi-particulate oral solid dose forms, are some of the advanceme nts. Such advancements have allowed for more flexibility of dose, easy administration, and improved medication formulation acceptance in pediatrics. In consideration of dosage forms for pediatrics, issues such as pediatric suitability, excipient selection, prospects for modified drug release formulations or fixed-dose combinations, palatability, and acceptability, as well as challenges were reviewed in the current manuscript.

Modeling of chitosan modified PLGA atorvastatin-curcumin conjugate (AT-CU) nanoparticles, overcoming the barriers associated with PLGA: An approach for better management of atherosclerosis

Conjugate drugs are evolving into potent techniques in the drug development process for enhancing the biopharmaceutical, physicochemical, and pharmacokinetic properties. Atorvastatin (AT) is the first line of treatment for coronary atherosclerosis; however its therapeutic efficacy is limited because of its poor solubility and fast pass metabolism. Curcumin (CU) is evidenced in several crucial signaling pathways linked to lipid regulation and inflammation. To enhance the therapeutic efficacy and physical properties of AT and CU, a new conjugate derivative (AT-CU) was synthesized and assessed by in silico, in vitro characterizations, and in vivo efficacy through mice model. Although the biocompatibility and biodegradability of Polylactic-co-Glycolic Acid (PLGA) in nanoparticles are well documented, burst release is a common issue with this polymer. Hence the current work used chitosan as a drug release modifier to the PLGA nanoparticles. The chitosan-modified PLGA AT-CU nanoparticles were prepaid by single emulsion and solvent evaporation technique. With raising the concentration of chitosan the particle size grew from 139.2 nm to 197.7 nm, the zeta potential rose from −20.57 mV to 28.32 mV, and the drug encapsulation efficiency improved from 71.81% to 90.57%. At 18 h, the burst release of AT-CU from PLGA nanoparticles was seen, hitting abruptly 70.8%. For chitosan-modified PLGA nanoparticles, the burst release pattern was significantly reduced which could be due to the adsorption of the drug on the surface of chitosan. The efficiency of the ideal formulation i.e F4 (chitosan/PLGA = 0.4) in treating atherosclerosis was further strongly evidenced by in vivo investigation.

A Review on Modified Release Dosage Form

Among the various routes of drug delivery oral route is most preferred route. But conventional dosage form offers few limitations which could be resolved by modifying the existing dosage form. Sustained and controlled drug delivery system helps in maintaining of constant plasma drug concentration and retards the release rate of drug thereby extending the duration of action. Modified release drug products allow at least a two-fold reduction in dosing when compared to a drug that is presented in a conventional immediate release form. Modified release drug products are designed to release active pharmaceutical ingredient over a longer duration of time; At least, longer than an Immediate release (I.R) formulation. Many Pharmaceutical companies also utilize the proprietary advantages of Modified release formulations to extend the patent life cycle of commercial products thereby bringing in new business.

EVALUATION OF VATERIA INDICA MODIFIED GUM AS A RELEASE RETARDANT MATRIX IN THE TABLET DOSAGE FORM

Objective: A natural gum from Vateria indica was investigated as a novel matrix-forming material for sustained drug delivery using diclofenac potassium as a model drug. Methods: In the current investigation, we formulated a matrix tablet using chloroform soluble gum portion of Vateria indica modified gum (VIMG) as a natural matrix-forming agent. It was used with a drug-polymer ratio ranging from 1:0.5 to 1:4.5. The pre-compression study of the powder blends was done by calculating bulk density, tapped density, angle of repose, and carr’s index, compressibility, and hausner’s ratio. The tablets were prepared by direct compression method and prepared tablets were evaluated and were found according to the official guidelines by pharmacopeia. The in vitro drug release was carried out using USP paddle type II apparatus and the release was found to be sustained. Results: The formulation VIMG-5 containing drug: polymer ratio 1:2.5 showed the 96.26%±1.73 drug release in 12 h. The results showed that chloroform soluble fraction of Vateria indica can be used as a drug release modifier to delay the rate of drug release, which depended on the amount of gum composition, as the concentration of gum was increased, there was sustained the drug release with promising accelerated stability. Conclusion: The evaluation studies on sustained release matrix tablets using Vateria indica chloroform soluble portion of gum as natural material demonstrate the multivariate applications such as matrix forming, binder, and release retardant of the gum in tablet formulation.

Formulation & development of fast dissolving film of Resperidone

Risperidone, an Antipsychotic drugs. Risperidone undergoes first pass metabolism on oral administration resulting in reduced bioavailability (60%). Thus the objective of the present study was to formulate and evaluate Fast Dissolving Film of Risperidone to overcome the limitation of bioavailability and increase patient’s compliance. In the present study Fast Dissolving Film were prepared by solvent-casting method using hydrophilic polymer HPMC K4M and PEG 400 as plasticizer. The eighteen formulations were prepared by the application of heat drying technique and evaluated for the fast dissolving films specification and characteristics. It was found that, the films has potential to modify drug release rate and possess good stability and less fragile property. The F9 batch of dried Fast Dissolving Film has shown promising drug release within 10 min (95.11%) and tensile strength.