Polymer Hydroxypropyl Methylcellulose Research Articles

Matrix effects in nilotinib formulations with pH-responsive polymer produced by carbon dioxide-mediated precipitation

Factors determining the pH-controlled dissolution kinetics of nilotinib formulations with the pH-titrable polymer hydroxypropyl methylcellulose phthalate, obtained by carbon dioxide-mediated precipitation, were mechanistically examined in acid and neutral environment. The matrix effect, modulating the drug dissolution, was characterized with a battery of physicochemical methodologies, including ToF-SIMS for surface composition, SAXS/WAXS and modulated DSC for crystallization characterization, and simultaneous UV-imaging and Raman spectroscopy for monitoring the dissolution process in detail. The hybrid particle formulations investigated consisted of amorphous nilotinib embedded in a polymer matrix in single continuous phase, displaying extended retained amorphicity also under wet conditions. It was demonstrated by Raman and FTIR spectroscopy that the efficient drug dispersion and amorphization in the polymer matrix were mediated by hydrogen bonding between the drug and the phthalate groups on the polymer. Simultaneous Raman and UV-imaging studies of the effect of drug load on the swelling and dissolution of the polymer matrix revealed that high nilotinib load prevented matrix swelling on passage from acid to neutral pH, thereby preventing re-precipitation and re-crystallization of incorporated nilotinib. These findings provide a mechanistic foundation of formulation development of nilotinib and other protein kinase inhibitors, which are now witnessing an intense therapeutic and industrial attention due to the difficulty in formulating these compounds so that efficient oral bioavailability is reached.

Optical humidity sensor using methylene blue immobilized on a hydrophilic polymer

An optical humidity sensor based on a membrane of hydrophilic polymer has been developed. It is a solid state sensor where the components of the membrane are hydrophilic polymer hydroxypropyl methylcellulose (HPMC), methylene blue to indicate humidity changes and a non-ionic surfactant. The mechanism of the sensor is based on the methachromasy related to the dimerization of methylene blue observed upon exposure to humidity. Measurement were carried out in the range of 0–99.5% relative humidity with a detection limit of 0.034%RH, showing a linear response, with good reproducibility (S.D. 0.27 at 1.78%RH, n=5) and stability, fast response and recovery times (60 and 90s, respectively) and reversibility up to 50% at room temperature (291K). This sensor displayed sufficient sensitivity that it could be used to detect low RH in environmental applications. Possible interferents were studied such as O2, CO2, CH4 and H2 gases, which did not show any interference whereas SO2 and H2S cause serious interferences on the humidity sensor.

Effect of gamma irradiation on HPMC/ZnO nanocomposite films

The present work looks into the structural, chemical, mechanical, optical and thermal modification in ZnO nanoparticle incorporated hydroxypropyl methylcellulose (HPMC) polymer films, induced by gamma irradiation. The irradiation process was performed in a gamma chamber at room temperature using Cobalt-60 source (average energy of 1.25 MeV) at different doses: 0, 50, 100, 150 and 200 kGy. The modifications in structural, chemical, mechanical, optical and thermal properties, due to gamma irradiation in HPMC/ZnO nanocomposite films, have been studied using wide angle X-ray scattering (XRD), Fourier transform infrared spectroscopy, universal testing machine, ultraviolet–visible spectrophotometry and thermogravimetric analysis. It is found that gamma irradiation improves the mechanical and thermal properties of nanocomposite films.

Formulation Development and Evaluation of Gabapentin Controlled Release Tablets

The objective of the present study was to develop a pharmaceutically equivalent, stable, robust, cost effective and quality improved formulation of Gabapentin controlled release tablets by using different grades of controlled release polymer. The design of dosage form was performed by choosing Hydroxypropyl Methyl Cellulose (HPMC K100MCR), Hydroxypropyl Methyl Cellulose (HPMC K15MCR), Microcrystalline Cellulose (MCC) and Di-calcium phosphate polymers as matrix builders. The drug-polymer compatibility studies were performed. Blend Uniformity was studied and accordingly the flowability was optimized for the powder blend. Tablets were prepared by direct compression with free flowing powder. The network formed by HPMC, MCC and DCP had been coupled satisfactorily with the controlled resistance, in vitro release and FT-IR. Mean dissolution time was also reported to compare various dissolution profiles. The formula was finalized by comparing the in vitro dissolution with that of the innovator SR and IR tablets. Optimized formulation of Gabapentin was formulated using 23% HPMC K100MCR and 10% of DCP. In vitro drug release profile was examined 98.69% within 12h. The releases of the formulation were fitting to Hixson Crowell model suggesting controlled zero order release from the formulation. The results suggested that direct compression is a suitable method to formulate controlled release Gabapentin tablets and it can perform therapeutically better than conventional immediate release dosage form.

Drug release behavior of polymeric matrix filled in capsule

A single unit sustainable drug release system was developed using hydroxypropyl methylcellulose (HPMC)-based matrices filled in capsule as the drug delivery device. Release behavior of propranolol HCl from these capsules was investigated and least square fitting was performed for the dissolution data with the different mathematical expressions. Effect of diluent, polymer, pH and hydrodynamic force on the drug release from the developed systems was investigated. The utilization of HPMC as a matrix former extended the drug release longer than 8h. HPMC viscosity grades affected the drug release, that is, increasing the amount of fillers such as lactose and dibasic calcium phosphate enhanced the drug release rate of HPMC matrices. The hydrodynamic force, type and amount of incorporated polymer apparently influenced the drug release. The physiochemical properties of polymers and interaction between HPMC and other polymers were important factors for prolongation of the drug release. The release mechanism from HPMC-based matrices in capsules was the non-Fickian transport in which the sustainable drug release of HPMC capsules could be achieved by the addition of polymeric matrix.

Zero‐order release three‐layered tablet with an acemetacin solid dispersion core and a hydroxypropyl methylcellulose capped matrix

ABSTRACTThe purpose of this study was to prepare a three‐layered tablet with hydroxypropyl methylcellulose (HPMC) polymers as a capped matrix to achieve a zero‐order release for acemetacin. As the middle active core, a solid dispersion in poly(vinyl pyrrolidone)–K30 polymers was manufactured via a solvent method to improve the solubility of acemetacin. A Box–Behnken design was used to optimize the formula, when the amounts of HPMC in the middle layer, HPMC in the external layer, and mannitol in the middle layer were chosen as the influencing factors. The dissolution profiles of the optimized formula exhibited superior fitting to the zero‐order release in 24 h. A bioavailability experiment was carried out by the administration of those three‐layered tablets to rabbits and their comparison with market Gaoshunsong controlled release capsules. The delayed time to reach the maximum plasma concentration, decreased the maximum plasma concentration, area under the plasma concentration‐time curve (0–48 h) AUC0–48, and area under the plasma concentration‐time curve (0–∞) AUC0–∞ were 9.33 ± 2.51 h, 8.59 ± 0.94 µg/mL, 200.81 ± 11.36 µg h/mL, and 212.902 ± 31.66 µg h/mL, respectively. © 2015 Wiley Periodicals, Inc. J. Appl. Polym. Sci. 2015, 132, 42059.

In-vitro and in-vivo evaluation of repaglinide loaded floating microspheres prepared from different viscosity grades of HPMC polymer

During the study repaglinide encapsulated floating microspheres were formulated and characterized for enhancing residence time of drug in git and thereby increasing its bioavailability. Floating microspheres of ethylcellulose (EC) and hydroxypropyl methyl cellulose (HPMC) (5 and 100cps) were prepared by emulsion solvent diffusion technique. During process optimization various parameters were studied such as: drug: polymer ratio, polymer ratio, concentration of emulsifier and stirring speed. Selected optimized formulations were studied for SEM, entrapment, floating behavior, drug release and kinetics. In-vivo floating ability (X-ray) study and in-vivo antidiabetic activity were performed on alloxan induced diabetic rats. Microspheres prepared with different viscosity grade HPMC were spherical shaped with smooth surface. Size of microspheres was in the range of 181.1–248μm. Good entrapment and buoyancy were observed for 12h. X-ray image showed that optimized formulation remained buoyant for more than 6h. Optimized formulation treated group shows significant (p<0.01) reduction in blood glucose level as compared to pure drug treated group. Repaglinide loaded floating microspheres expected to give new choice for safe, economical and increased bioavailable formulation for effective management of NIDDM.

An appraisal of innovative meloxicam mucoadhesive films for periodontal postsurgical pain control: A double-blinded, randomized clinical trial of effectiveness.

Background and Objective:Transmucosal analgesic delivery is a promising approach to periodontal postoperative pain management. The purpose of this clinical trial is to appraise the effectiveness of transmucosal drug delivery system with meloxicam films and to identify its minimum effective dosage via this route after periodontal flap surgery.Materials and Methods:The analgesic mucoadhesive films were formulated using meloxicam and hydroxypropyl methyl cellulose polymer by solvent casting method. The sample size consisted of 60 chronic periodontitis patients who require periodontal flap surgery. The subjects were randomized using lottery method into four groups (Group A - 45 mg; B - 30 mg; C - 20 mg; D - 10 mg meloxicam per film). After periodontal flap surgery, the respective meloxicam mucoadhesive films were placed over the surgical site and were removed on 4th day of postsurgery. The primary outcome measure was postsurgical pain level and recorded at 1st, 2nd, 3rd, 4th, 5th, 24th, and 48th h using a 0–10 mm visual analog scale with markings from 0 = no pain to 10 = extreme pain.Results:The postoperative pain control observed in Groups A and B was found to be effective, and the patient comfort level was very satisfactory. Whereas in Group C, it was found to be high in the first 3 h postsurgically, after which adequate pain relief was seen. Group D exhibited inadequate pain relief. No adverse reactions were noted after applying the film in any of the groups.Conclusion:Transmucosal delivery of meloxicam was found to be effective and safe in postsurgical pain control of periodontal flap surgery. The minimum effective dosage via this route for meloxicam was found to be with 30 mg mucoadhesive films.

Formulation and Evaluation of Cefixime Trihydrate Matrix Tablets Using HPMC, Sodium CMC, Ethyl Cellulose.

The objective of the present work is to design sustained release matrix tablets of cefixime trihydrate by incorporating drug in a matrix made up of release retardant polymers, which prolong drug release leading to minimization of the peak and valley effect in the plasma and provide patient convenience. The effect of combination of polymers on parameters like release pattern, release mechanism of the drug were studied. Total nine formulations each containing 200 mg of drug were prepared by direct compression method. The formulations F-1, F-2, F-3 were prepared with a 1:1 drug to polymer ratio using hydroxypropyl methylcellulose, carboxymethyl cellulose sodium and ethyl cellulose. F-4 was prepared with a 1:1 ratio of hydroxypropyl methylcellulose, carboxymethyl cellulose sodium, F-5 as prepared with a 1:1 ratio of hydroxypropyl methylcellulose and ethyl cellulose, F-6 was prepared with a 1:1 ratio of carboxymethyl cellulose sodium and ethyl cellulose, F-7, F-8, F-9 were prepared by using polymers hydroxypropyl methylcellulose, carboxymethyl cellulose sodium and ethyl cellulose in the ratios of 0.5:0.5:1, 0.5:1:0.5, and 1:0.5:0.5. Designed matrix tablets were evaluated for various pre-compression and post-compression parameters. Formulation F-5 showed 102.15 % release at the end of 12 h and it is selected as the best formulation. All Formulations followed zero order with non-Fickian diffusion method.

Formulation of Sustained Release Floating Microspheres of Furosemide from Ethylcellulose and Hydroxypropyl Methylcellulose Polymer Blends

Furosemide is a potent and commonly used loop diuretic. It is absorbed largely in the stomach and upper small intestine. This narrow absorption window is responsible for its low bioavailability of about 50%, and variable and erratic absorption. The objective of the present investigation was to formulate and evaluate floating microspheres of furosemide for prolonged buoyancy with sustained delivery of the drug into the gastric content. Furosemide loaded microspheres were prepared by the solvent evaporation method. The drug entrapment efficiency was high for all of the formulations ranging from 86.2 to 98.4%. The yield of microspheres production was good partticularly at increased EC/HPMC ratio and lower temperatures. Drug amount and EC/HPMC ratio showed highly significant effects (p<0.0001) on cumulative drug release and buoyancy of microspheres. Floating microspheres that effectively sustain the drug release more than 12 h and exhibit buoyancy of greater than 77% in 12 h were developed. Finally the study confirmed that various furosemide loaded EC/HPMC microspheres formulations could be developed that effectively sustain the drug release for a desired period by varing the ratio of EC and HPMC, and drug amount.

Determining the polymer threshold amount for achieving robust drug release from HPMC and HPC matrix tablets containing a high-dose BCS class I model drug: in vitro and in vivo studies.

It is challenging to achieve mechanically robust drug-release profiles from hydrophilic matrices containing a high dose of a drug with good solubility. However, a mechanically robust drug release over prolonged period of time can be achieved, especially if the viscosity and amount of the polymer is sufficiently high, above the "threshold values." The goal of this research was to determine the hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose (HPMC) polymer threshold amount that would enable robust drug release from matrix tablets containing a high dose of levetiracetam as a class I model drug according to the Biopharmaceutical Classification System (BCS). For this purpose, formulations containing HPC or HPMC of similar viscosity range, but in different amounts, were prepared. Based on the dissolution results, two final formulations were selected for additional in vitro and in vivo evaluation to confirm the robustness and to show bioequivalence. Tablets were exposed to various stress conditions in vitro with the use of different mechanically stress-inducing dissolution methods. The in vitro results were compared with in vivo results obtained from fasted and fed bioequivalence studies. Under both conditions, the formulations were bioequivalent and food had a negligible influence on the pharmacokinetic parameters C max and area under the curve (AUC). It was concluded that the drug release from both selected formulations is mechanically robust and that HPC and HPMC polymers with intrinsic viscosities above 9 dL/g and in quantities above 30% enable good mechanical resistance, which ensures bioequivalence. In addition, HPC matrices were found to be more mechanically robust compared to HPMC.

Evaluating sulfuric acid reduction, substitution, and recovery to improve environmental performance and biogas productivity in rubber latex industry

Sulfuric acid is heavily used in concentrated rubber latex factories to coagulate rubber particles in skim latex. The resulting sulfate-rich wastewater creates the onset of toxic H2S gas production in the wastewater holding ponds, causing severe corrosion to materials and community disturbance when dispersed to ambient air. This work identified and evaluated measures to reduce H2S production by minimizing sulfate concentration in the wastewater. Sulfuric acid use could be cut down by pre-removal of ammonia in the skim latex as well as a stricter manipulation of acid dosing. In search of a more benign chemical, a heat sensitive polymer was identified and tested as sulfuric acid substitute. The use of hydroxypropyl methylcellulose polymer (HPMC) changed wastewater characteristics and was found to increase biogas production approximately by 2.4 times in batch assay at the initial pH 7.0 and methane yield by 2.7 times in continuous digester operation at HRT 7 days. Finally, a resource recovery option was evaluated. The remaining H2S in the produced biogas was oxidized in the biotrickling filter to sulfuric acid that has a potential to partially supplement the fresh acid. This work demonstrated an integrated approach in waste management to improve environmental performance, safety and energy recovery in the concentrated latex industry.

Study of the Homogeneity of Drug Loaded in Polymeric Films Using Near-Infrared Chemical Imaging and Split-Plot Design

Split-plot design (SPD) and near-infrared chemical imaging were used to study the homogeneity of the drug paracetamol loaded in films and prepared from mixtures of the biocompatible polymers hydroxypropyl methylcellulose, polyvinylpyrrolidone, and polyethyleneglycol. The study was split into two parts: a partial least-squares (PLS) model was developed for a pixel-to-pixel quantification of the drug loaded into films. Afterwards, a SPD was developed to study the influence of the polymeric composition of films and the two process conditions related to their preparation (percentage of the drug in the formulations and curing temperature) on the homogeneity of the drug dispersed in the polymeric matrix. Chemical images of each formulation of the SPD were obtained by pixel-to-pixel predictions of the drug using the PLS model of the first part, and macropixel analyses were performed for each image to obtain the y-responses (homogeneity parameter). The design was modeled using PLS regression, allowing only the most relevant factors to remain in the final model. The interpretation of the SPD was enhanced by utilizing the orthogonal PLS algorithm, where the y-orthogonal variations in the design were separated from the y-correlated variation.

PH-responsive thiolated chitosan nanoparticles for oral low-molecular weight heparin delivery: in vitro and in vivo evaluation

The aim of present study was to investigate a pH-responsive and mucoadhesive nanoparticle system for oral bioavailability enhancement of low-molecular weight heparin (LMWH). The thioglycolic acid (TGA) was first covalently attached to chitosan (CS) with 396.97 ± 54.54 μmol thiol groups per gram of polymer and then the nanoparticles were prepared with thiolated chitosan (TCS) and pH-sensitive polymer hydroxypropyl methylcellulose phthalate (HPMCP) by ionic cross-linking method. The obtained nanoparticles were characterized for the shape, particle size, zeta potential, drug entrapment efficiency and loading capacity. In vitro results revealed the acid stability of pH-responsive nanoparticles, which had a significant control over LMWH release and could effectively protect entrapped drugs in simulated gastric conditions. By the attachment of the thiol ligand, an improvement of permeation-enhancing effect on freshly excised carp intestine (1.86-fold improvement) could be found. The mucoadhesive properties were evaluated using fluorescently labeled TCS or CS nanoparticles. As compared with the controls, a significant improvement of mucoadhesion on rat intestinal mucosa was observed in TCS/HPMCP nanoparticles via confocal laser scanning microscopy. The activated partial thromboplastin time (APTT) was significantly prolonged and an increase in the oral bioavailability of LMWH was turned out to be pronounced after oral delivered LMWH-loaded TCS/HPMCP nanoparticles in rats, which suggested enhanced anticoagulant effects and improved absorption of LMWH. In conclusion, pH-responsive TCS/HPMCP nanoparticles hold promise for oral delivery of LMWH.

Effects of CdCl2 concentration on the structural, thermal and ionic conductivity properties of HPMC polymer electrolyte films

The present study illustrates cadmium chloride (CdCl2)-doped hydroxypropyl methylcellulose (HPMC) polymer electrolyte films. Solution cast method is employed to prepare polymer electrolyte samples of HPMC complexed with various concentrations of CdCl2 (1–4 %, wt.%). Structural and thermal studies of these polymer samples were investigated using X-ray diffraction (XRD) and differential scanning calorimetry (DSC). XRD results showed that the amorphous domains of HPMC polymer matrix were increased with increase in CdCl2 salt concentration. DSC results revealed that the presence of CdCl2 in the polymer matrix increases the melting temperature; however, it is observed that the heat of fusion (ΔH f ) is high for pure HPMC films. The variation in the film morphology was examined by scanning electron microscopy (SEM). Direct current (dc) conductivity was measured in the temperature range 313–383 K. The magnitude of electrical conductivity was found to be increased with increasing salt concentration and temperature. The activation energy region data (region I and region II) indicated the dominance of ion-type charge transport in these polymer electrolyte films. HPMC polymer electrolytes with 4 % CdCl2 salt concentration exhibit the least crystallinity and the highest conductivity 1.01 × 10−6 Scm−1 at 313 K.

Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori

Gastroretentive levofloxacin (LVF) floating mini-tablets for the eradication of Helicobacter pylori (H. pylori) were prepared using the matrix forming polymer hydroxypropyl methylcellulose (HPMC K100M), alone or with Carbopol 940P in different ratios by wet granulation technique. Buoyancy of mini-tablets was achieved by an addition of an effervescent mixture consisting of sodium bicarbonate and anhydrous citric acid to some formulations. The prepared mini-tablets were evaluated for weight variation, thickness, friability, hardness, drug content, in vitro buoyancy, water uptake and in vitro release. The optimized formula was subjected to further studies: FT-IR, DSC analysis and in vivo examination in healthy volunteers. The prepared mini-tablets exhibited satisfactory physicochemical characteristics. Incorporation of gas-generating agent improved the floating parameters. HPMC K100M mini-tablet formulation (F1) offered the best controlled drug release (>8h) along with floating lag time <1s and total floating time >24h. The obtained DSC thermograms and FT-IR charts indicated that there is no positive evidence for the interaction between LVF and ingredients of the optimized formula. The in vivo test confirmed the success of the optimized formula F1 in being retained in the stomach of the volunteers for more than 4h. LVF floating mini-tablets based on HPMC K100M is a promising formulation for eradication of H. pylori.

Pharmacokinetics and analgesic effect of ketorolac floating delivery system

Objectives: The efficacy of ketorolac tromethamine (KT) floating alginate beads as a drug delivery system for better control of KT release was investigated. The formulation with the highest drug loading, entrapment efficiency, swelling, buoyancy, and in vitro release would be selected for further in vivo analgesic effect in the mice and pharmacokinetics study in rats compared to the tablet dosage form.Methods: KT floating alginate beads were prepared by extrusion congealing technique. KT in plasma samples was analyzed using a UPLC MS/MS assay.Results: The percentage yield, drug loading and encapsulation efficiency were increased proportionally with the hydroxypropylmethyl cellulose (HPMC) polymer amount in the KT floating beads. A reverse relationship was observed between HPMC amount in the beads and the KT in vitro release rate. F3-floating beads were selected, due to its better in vitro results (continued floating for >8 h) than others. A longer analgesic effect was observed for F3 in fed mice as compared to the tablets. After F3 administration to rats, the Cmax (2.2 ± 0.3 µg/ml) was achieved at ∼2 h and the decline in KT concentration was slower. F3 showed a significant increase in the AUC (1.89 fold) in rats as compared to the tablets.Conclusion: KT was successfully formulated as floating beads with prolonged in vitro release extended to a better in vivo characteristic with higher bioavailability in rats. KT in floating beads shows a superior analgesic effect over tablets, especially in fed mice.

Effects of CdCl2 concentration and gamma irradiation on the structural, thermal and electrical conductivity properties of HPMC polymer electrolyte films

Solid polymer electrolyte films based on hydroxypropyl methylcellulose (HPMC) with different concentrations of cadmium chloride (CdCl2) were prepared by solution cast method. Different techniques has been employed to investigate the effects of structural, thermal and ionic conductivity behavior of these polymer electrolyte films upon gamma irradiation with different doses of 20, 60 and 100 kGy. The dissolution of the salt into the polymer host and the structural properties of pure and CdCl2 (1% - 4%) (wt. %) complexed HPMC polymer electrolyte films before and after irradiation was confirmed by X - ray diffraction (XRD) studies. XRD results revealed that the amorphous domains of HPMC polymer matrix was increased with increase in the salt concentration and with the gamma dose. The percentage of crystallinity is found to be high in pristine unirradiated HPMC films. The thermal properties of these polymer electrolyte films before and after irradiation were studied using differential scanning calorimetry (DSC). The results revealed that the presence of CdCl2 in the polymer matrix increases the melting temperature, however it is observed that the total enthalpy of fusion ( ) is maximum for unirradiated pristine HPMC films. The variation of film morphology was examined by scanning electron microscopy (SEM). Direct current (dc) conductivity was measured in the temperature range of 313-383K. The magnitude of conductivity was found to increase with increasing concentration of the salt, temperature and for higher dose of radiation. The composition HPMC:CdCl2 (5:4) for unirradiated and irradiated samples, found to exhibit the least crystallanity and the highest conductivity.

English

The use of polymer in cement slurry is necessary to retain viscosity at ambient temperature and thermal thickening properties with increasing temperature. Current polymers, polysaccharides and their derivatives are extensively studied. At high temperature these polymers do not yield thickening of viscosity, but exhibit loss of slurry and gas migration. Therefore, this study presents hydroxypropylmethylcellulose (HPMC) polymer as a viscosifying agent in cement slurry. The HPMC possesses a strong thermal thickening and solid suspension ability which means low viscosity at ambient temperature and viscosity increase with respect to temperature. Thus, a series of experiments was conducted on HPMC polymer as a viscosifying agent in cement slurry. Different concentrated solutions were prepared (i.e. 1.5 to 2.5 wt%), in order to characterize their viscosity with respect to shear rate and increasing temperature up to 100°C. Then, cement slurries were prepared with HPMC as the primary viscosifier, to determine the rheological properties at high temperatures. It was observed that HPMC polymer has increased viscosity from 90°C to 100°C. The improved rheology of cement slurry, in terms of plastic viscosity and yield point at different concentrations, revealed HPMC as a capable viscosifying agent at high temperature. Moreover, increased gel strength with increasing concentration was also observed, which may cause a higher pumping rate on the surface. It was concluded that HPMC polymer acts as a viscosifying agent at high temperature. HPMC-based slurries showed high rheology (plastic viscosity and yield point) with HPMC polymer. Thus, the use of this additional additive should be considered in the design of appropriate cement slurry.

FORMULATION AND IN-VITRO EVALUATION OF ZOLMITRIPTAN IN SITU GEL FOR NASAL ADMINISTRATION

The aim of present investigation was formulation and in-vitro evaluation of in situ gel for the nasal delivery of zolmitriptan. The in situ gel was prepared by temperature induced gelation technique using Pluronic with mucoadhesive polymer hydroxy propyl methyl cellulose K4 M in different ratios. The in situ gels so prepared were characterized and from the evaluation studies, batch PH2 was optimized and further subjected for stability studies at 30±2°C and 60±5% RH for 90 days. These formulations retained good stability at accelerated conditions and also did not show any remarkable damage to nasal mucosa in histopathological study. Owing to these properties it can be used as an effective delivery system for the nasal route.