HPMC Concentration Research Articles

FORMULATION OPTIMIZATION AND EVALUATION OF MOUTH DISSOLVING FILM OF RAMOSETRON HYDROCHLORIDE

Objective: Ramosetron Hydrochloride is found to be more potent and having a longer duration of action with the least side effects, but the major drawback is it undergoes hepatic first-pass metabolism so our aim is to prepare mouth dissolving film (MDF) of Ramosetron hydrochloride for rapid relief in emesis.
 Methods: The mouth dissolving films of Ramosetron Hydrochloride were prepared by using the solvent casting method. Films were formulated using HPMC E5 (Hydroxy Propyl Methyl Cellulose) as a film-forming agent, PEG400 (Polyethylene glycol) as a plasticizer and Aspartame as the sweetening agent. A 32 full factorial design was applied considering the concentration of HPMC E5 (X1) and concentration of PEG400 (X2) as independent variables and % cumulative drug release (Y1) (CDR), disintegration time (Y2) (DT) and tensile strength (Y3) (TS) as dependent variables. The prepared films were evaluated for thickness, folding endurance, tensile strength, disintegration time, drug content uniformity and taste masking by E-tongue. The results indicated that factors X1 and X2 were found to be having a positive effect on DT and TS and negative effects on CDR.
 Results: The optimized formulation was found to be the best with 94.00±0.85% in vitro drug release, 33.22±0.75 sec DT and 1.359±0.005 g/mm2 tensile strength. Concentration of aspartame was optimized with E-tongue taking into consideration increased electric potential with decreasing bitterness.
 Conclusion: Thus, a rapidly dissolving oral film of Ramosetron Hydrochloride with successful taste masking and immediate in vitro drug release was prepared using a solvent casting technique.

Formulation and Evaluation of Pseudoephedrine Hydrochloride Loaded Alginate Microbeads

Multiple unit dosage forms such as microbeads have increased acceptance because of added even spreading of the drug in the gastrointestinal tract, unvarying drug absorption, abridged local irritation and removal of undesirable intestinal retaining of polymeric material, when compared to non-disintegrating single unit dosage form. The purpose of the presented research is to develop microbeads of pseudoephedrine hydrochloride utilizing sodium alginate as the hydrophilic carrier in combination with HPMC as drug release modifier to lessen the dosing frequency and thereby advance the patient compliance. The microbeads were formulated by varying concentrations of HPMC and calcium chloride. The optimum formulation was chosen based upon in vitro drug release studies and further evaluated. The compatibility of drug-polymer was studied using FTIR analysis. The prepared formulation underwent evaluation for various parameters like drug entrapment, microbeads size, swelling index, mucoadhesive property and stability. No significant drug-polymer interactions were observed in compatibility studies and the formulation was found to be stable on 45 days storage. The formulations exhibited an extended drug release pattern which was the ultimate aim of the study. The microbeads represented good yield, high drug entrapment, low microbeads size and appropriate swelling property. The in vitro wash-off test indicated that the sodium alginate microbeads represent decent mucoadhesive properties. Henceforth, the formulated HPMC coated sodium alginate beads can be utilized as a substitute and cost-effective carrier for the oral controlled delivery of pseudoephedrine hydrochloride.
 Keywords: microbeads, pseudoephedrine hydrochloride, sodium alginate, drug release

Formulation and evaluation of floating mucoadhesive microspheres loaded with antiulcer drug

The objective of the present study was to formulate and evaluate Floating-mucoadhesive microspheres which is loaded with famotidine for the treatment of Helicobacter pyloric (H. pylori) infection. Formulation of Gastro - Retentive Dosage Forms (GRDFs) containing suitable drug candidate which would remain in stomach and/or upper part of GIT for prolonged period of time thereby is maximizing the drug release at desired site within the time before GRDFs leave the stomach and or upper part of GIT. Tablets were prepared by Ionic gelation method by using the polymers such as HPMC K4m, ethyl cellulose, sodium alginate, calcium chloride and by keeping the concentration of HPMC, sodium alginate, calcium chloride were constant and five formulation were prepared was evaluated for drug - excipient compatibility, density, buoyancy test, mucoadhesion force, percentage yield, entrapment efficiency, particle size and in-vitro release profile and stability studies of optimized formulation. Analysis of drug release from tablet indicates drug release by zero order rate kinetics. No significant change was observed in physical appearance, drug content, floatability or in vitro dissolution pattern after storage at 40°C±2°/75% RH for six months. Formulation no: 5 was found to be the optimized one which is satisfying all the required specifications.

Design and optimization of film-forming gel of etoricoxib using research surface methodology.

The present investigation is focused on the development of transdermal film-forming gel (FFG) loaded with etoricoxib employing research surface methodology (RSM). Box-Behnken surface design method was used to develop experimental run using different concentrations of etoricoxib, hydroxypropyl methylcellulose (HPMC K100M), and eudragit RL100 as independent variables, and Derringer's optimization tool was employed to optimize best possible formulation. The dependent variables considered in this study were viscosity and drug permeation at 24 h (Q24, μg/cm2). Anti-inflammatory study was performed on Wistar albino rats for 8 h. Skin irritation studies and accelerated stability studies were performed for validated FFG formulations. Quadratic model was found to be best fit model (p < 0.0001) for both the responses. The influence of HPMC concentration on the viscosity was found to be highest whereas concentration of etoricoxib was maximum for Q24. The optimum composition of the FFG was observed to be 4% of etoricoxib, 1.1246% of HPMC, and 0.4% of eudragit. Above composition resulted in viscosity of 1549.5 mPa.s and maximum Q24 of 4639.11 μg/cm2 with desirability 0.918. The in vivo anti-inflammatory study demonstrated better sustained release effect (for 8 h) of optimized FFG compared to orally administered drug suspension. An average irritation score of 0.555 was observed on Draize scoring system. The validated FFG formulation was found to be stable for the 3 months in accelerated conditions. It can be concluded from the above investigations that the validated FFG formulation of etoricoxib is well tolerated and could provide sustained drug release for 8 h. Graphical abstract.

Optimized chronomodulated dual release bilayer tablets of fexofenadine and montelukast: quality by design, development, and in vitro evaluation

BackgroundThe conventional oral dosage forms are not effective in dealing with chronopathological conditions, such as nocturnal asthma. Therefore, there is an unmet need to develop a delivery system that can deliver drug as per the chronopharmacology of the diseases. The purpose of the study is to use quality by design (QbD) technique and pulsatile principles for the development of Eudragit-coated dual release bilayer tablets. The dual layer consists of immediate release layer of fexofenadine HCl and sustained release layer of montelukast sodium.ResultsThe quality target product profile of the formulation was developed, and the critical quality attributes were identified. Three-level, three-factor Box-Behnken design was used for the optimization of the bilayer tablets. Based on the design, a total of 13 formulation combinations (F1–F13 and M1–M13) were made having acceptable micromeritic properties. The developed immediate and sustained release layers were evaluated for physicochemical properties. Depending upon the value of the diffusion exponent, the Fickian diffusion mechanism is dominant among immediate and sustained release tablet layers. Response curve for immediate release layer showed that concentrations of sodium starch glycolate and sodium bicarbonate had a negative effect on disintegration time and a positive effect on drug release. For sustained release tablet layer, concentrations of HPMC E 5 LV and magnesium stearate had a significant effect on drug release. The ANOVA and diagnostic plots confirmed the significance and goodness of fit of the used model. Based on desirability plot values, optimized formulation was developed and coated with Eudragit coat. The coated bilayer tablet showed met the requirement of providing an immediate release during the first hour and a sustained release action for a period of more than 8 h after passing the gastric region.ConclusionsThe formulation can be fruitful in curbing the menace of nocturnal asthma and providing a high degree of patient compliance as the patient will not have to wake up at night to take the medication.

QSPR Modeling of Biopharmaceutical Properties of Hydroxypropyl Methylcellulose (Cellulose Ethers) Tablets Based on Its Degree of Polymerization.

Quantitative structure-property relationship (QSPR) approach has been widely used in predicting physicochemical properties of compounds. However, its application in the estimation of formulation properties based on the polymer used in it to achieve desired formulation characteristics is an extremely challenging process. In the present research, predictive QSPR models were developed by correlating the physicochemical properties of varying grades of cellulose ethers (hydroxypropyl methylcellulose, HPMC) with those of nateglinide (NTG) containing tablets (in vitro and in vivo properties). Sustained release tablets of NTG were prepared by using different grades and concentrations of HPMC and subsequently characterized for in vitro as well as in vivo parameters. Further, QSPR models for individual formulation property were developed by correlating the polymeric physicochemical properties with the formulation characteristics. Subsequently, a true external validation method was used to validate the predictability of developed models. The dissolution study indicated Korsmeyer-Peppas as the best fit model following non-Fickian as drug transport mechanism extending the drug release up to 12h. In vivo studies showed limited absorption of the NTG. Developed QSPR models showed promising validated predictability for formulation characteristics. The applicability of present work in formulation development could significantly reduce the time and cost expenditure on design trials without actually formulating a delivery system.

Optimasi Formula Masker Gel Peel Off Ekstrak Buah Mahkota Dewa (Phaleria macrocarpa (Scheff.) Boerl ) Dengan Variasi PVA Dan HPMC Menggunakan Metode Simplex Lattice Design

&#x0D; &#x0D; &#x0D; &#x0D; Mahkota Dewa (Phaleria macrocarpa (Scheff.) Boerl) is an effectiveplant against bacteria the causes of acne. To facilitate the application, it formulated in a peel off gel mask preparation. This study aims to determine the effect of the concentration of PVA as film forming and HPMC as a gelling agent on the physical properties of the peel off gel mask and determine the concentration of PVA and HPMC which produce the optimum formula.The Mahkota Dewa fruit was extracted by soxletation with ethanol 70%. The extract was made into 5 runs with variations in the concentration of PVA (10-16%) and HPMC (2-4%). The fifth run in the test of physical properties include organoleptic tests, homogenity, pH, viscosity, spreadability, adhesion and drying time. The optimum formula of peel off gel mask is obtained from software design expert version 6.0.8. simplex lattice design method with the studied response to viscosity, spreadability, and drying time.The results show that increasing the concentration of PVA can increase viscosity and drying time, and increasing the concentration of HPMC can increase the value of dispersion of the preparation. The optimum formula was obtained with a variation of PVA 13.09% and HPMC of 2.97%.&#x0D; &#x0D; &#x0D; &#x0D;

Development of optimized mucoadhesive thermosensitive pluronic based in situ gel for controlled delivery of Latanoprost: Antiglaucoma efficacy and stability approaches

This work was investigated to formulate an optimized in situ gel of Latanoprost depending on a sol-to-gel transition system upon ocular instillation. The in situ gelling system could overcome the lachrymal drainage, low corneal permeability, poor availability and low therapeutic efficiency revealed by the conventional ophthalmic preparations. An optimal factorial design was built to study the impact of four factors (P127 concentration, P68 concentration, grade and concentration of HPMC) on the temperature of sol-gel transition, mucoadhesion properties and strength of the gel. The prepared formulations were also evaluated for viscosity, pH, in vitro drug release, ex vivo permeability. Stability studies were carried out for the selected formula at different temperatures (4 °C, 25 °C and 35 °C). The anti-glaucoma efficiency of the optimized formula was estimated using an induced glaucoma model in rabbits. The optimum formula revealed sol-gel temperature of 34.3 °C, gel strength of 23.13 g, mucoadhesionof 0.06 m J and high flux of 11.4 μg/cm2/hr. The anti-glucoma efficiency of the in situ gel formulation was 2.9 fold increase compared to eye drop. It also revealed a rapid decrease in Intraocular Pressure (IOP) within 30 min after administration that extended to 8 h compared to the conventional eye drop which showed gradual decrease in IOP that extended for only 3 h. Latanoprost loaded in situ gelling system is more stable at the different temperatures than the traditional eye drop. This developed Latanoprost thermosensitive in situ gel may provide a non-invasive alternative to the conventional anti-glaucoma eye drop.

Formulasi Dan Uji Aktivitas Anti Bakteri Masker Gel Peel-Off Ekstrak Daun Pacar Air (Impatiens balsamina linn.) Dengan Kombinasi Basis PVA dan HPMC

Peel-off gel mask is one of the practical masks, because after dry the mask can be directly removed without rinsing. In this research, a peel-off gel mask formulation from a pacar air leaf extract (Impatiens balsamina Linn.) Has antibacterial activity against Staphylococus Aureus bacteria. The peel-off gel mask is prepared in 3 formulas by varying the PVA and HPMC concentrations of F1 (1: 2,6), F2 (1: 3), F3 (1: 3,5). Evaluation of gel quality used is organoleptic test, viscosity, adhesion, drying time, dispersion, pH. Testing of antibacterial activity was done by using the diffusion method of wells. The positive control used was clindamycin phosphate 1.2%, the negative control used was the base of the peel-off gel mask. Results of physical evaluation and antibacterial activity test were analyzed using SPSS software with trust level of 0.05. Based on the results obtained F3 is the optimum formula, because F3 has a corresponding pH of 5.2 ± 0.10, the corresponding depth of 6.85 ± 0.13, the fastest drying time of 21.68 ± 0.33 and the anti-activity the best bacteria. Based on testing of antibacterial activity of F1, F2 and F3 have antibacterial activity against Staphylococus Aureus bacteria.

Sensitivity of a continuous hot-melt extrusion and strand pelletization line to control actions and composition variation

The purpose of this work was to develop a robust hot-melt extrusion and strand pelletization process for manufacturing pellets with an immediate release (IR) of a poorly water-soluble active pharmaceutical ingredient (API), nimodipine. The robustness of pharmaceutical continuous manufacturing processes and of its control strategy is vital for competitiveness to traditional batch-manufacturing. Therefore, first the sensitivity of product quality, process stability, and process monitoring tools to i) parameter changes due to control actions and ii) typical process deviations, i.e., feeding errors, was investigated in a design of experiments (DoE). Thereby, die melt pressure was found to be highly sensitive to composition deviations, i.e. a limiting factor for process stability. Especially critical were deviations to increased HPMC content, since it behaved as a filler in the melt. Pelletization, or pellet size and size distribution respectively, were found to be sensitive to an increased throughput, due to the resulting insufficient strand cooling before the pelletizer. API dissolution in contrast, was found to be robust across the entire investigated range of formulation and process settings. Second, a design space for the production of IR pellets for subsequent tableting was established, and finally, a technical control strategy was developed to ensure a robust process. Near-infrared (NIR) spectroscopy was applied to monitor API content and the sensitivity of the residence time distribution (RTD) was investigated by means of tracer measurements. NIR-based API content monitoring and RTD models for material tracking were found to be at risk after processing melt with high HPMC content, due to a lack of purging by less viscous formulation compositions.

DESIGN, CHARACTERIZATION AND STATISTICAL OPTIMIZATION OF RAMOSETRON HYDROCHLORIDE MOUTH DISSOLVING FILM USING DESIGN OF EXPERIMENT

Objective: The present study aims to prepare a mouth dissolving film of ramosetron hydrochloride to provide relief to cancer patients suffering from nausea and vomiting.&#x0D; Methods: Mouth dissolving film of ramosetron hydrochloride were prepared and optimized using three levels two factor design. The films were prepared using the solvent casting technique. The effect of formulation variables such as the concentration of HPMC E15, and honey on disintegration time, tensile strength and drug release from the film were studied. The films were evaluated for weight, thickness, folding endurance, tensile strength, percent elongation, surface pH, disintegration time and drug release.&#x0D; Results: All the films were found to be transparent, non-sticky and easily peelable. The concentration of HPMC E 15 and Honey was found to have a significant effect on disintegration time and drug release of the mouth dissolving film. Formulation R1 was found to the best formulation with 104.21 % release in 9 min and disintegration time of 57 seconds.&#x0D; Conclusion: It can be concluded that the developed mouth dissolving film could serve as an effective, convenient alternative to prevent nausea and vomiting in cancer patients of any age group.

Characterization of sodium caseinate/Hydroxypropyl methylcellulose concentrated emulsions: Effect of mixing ratio, concentration and wax addition.

The effects of mixing ratio (1:1, 2:1 and 4:1 sodium caseinate: Hydroxypropyl methylcellulose, CN:HPMC), HPMC concentration (0, 0.6 and 1.2 wt%), CN concentration (0, 1.25 and 2.5) and beeswax addition (3%) on the physical stability of concentrated O/W emulsions (φoil = 0.6) were investigated. The emulsion stability, particle size distribution, microstructure and rheological properties were measured. The results showed that emulsion stability was significantly improved with increasing HPMC concentration (pvalue < 0.05). The samples with the highest and the lowest biopolymers concentration at mixing ratio of 2:1 had the highest and the lowest ESI (98% and 48%), respectively. In addition, the most stable sample had the smallest volume mean diameter and approximately desirable rheological properties. The beeswax addition considerably improved rheological properties whereas increased droplets diameter and emulsion instability. In summary, concentrated emulsions stabilized by caseinate/Hydroxypropyl methylcellulose complex may be useful for application in particular food such as heavy cream, mayonnaise, oleogels and pharmaceutical products.

Gel Formulation of Lemongrass Essential Oil with HPMC and Carbopol Bases

Lemongrass (Cymbopogon citratus) essential oil is proven to have efficacy as an antibacterial against pathogenic bacteria, such as Staphylococcus aureus. Essential oils was formulate into gel dosage forms with a base combination of HPMC and carbopol. The use of this combination is known to produce a gel with physical properties better than a single use. This research aimed to investigate the effect of variations of HPMC and carbopol to the physical properties of the gel, the concentration of HPMC and carbopol to produce the optimum formula, and the physical stability of essential oil gel of lemongrass during storage. Gel was made by lemongrass essential oil at a concentration of 6% with base of HPMC and carbopol. Each formula were made and tested the physical properties that include organoleptic, homogenity, pH, viscosity, spreadability and adhesiveness. HPMC and carbopol composition were determined through the process of screening and optimization Simplex Lattice Design methods by Design Expert 7.1.5 software. Experimental results and predictions of SLD were verified by testing one sample t-test with a 95% confidence level. The optimum formula gel of lemongrass essential oil consisting of 4.00% HPMC and 1.00% carbopol. The results test of physical properties of lemongrass essential oil gel obtained homogeneous gel with a pH value of 6.00 ± 0.00, viscosity of 280.00 ± 26.46 dPa.S, spreadability of 9.36 ± 0.47 cm2, and adhesiveness of 2.36 ± 0.10 seconds. Lemongrass essential oil gel was stable for 3 cycles of testing include organoleptic, homogeneity, syneresis, pH, adhesion, and the viscosity of the gel. Spreadability of gel was not stable.

Biomimetic mineralization of the carbonates regulated by using hydroxypropyl methylcellulose macromolecules as organic templates

Control of the morphology of carbonate crystals plays an indispensable role in mineralization process. We investigated the relationship between HPMC concentration and different molar ratios of Mg/Ca on the carbonate crystallization by monitoring crystal polymorph, crystal size, and morphology. In this experiment, the total molars of [Mg2+] and [Ca2+] were 50 mM. The results demonstrated that different molar ratio of Ma/Ca primarily can help different morphology form in multidimensional spline space, for instance, lens-like calcite, spindle shaped aragonite and polyhedron nesquehonite. Moreover, the metastable aragonite phase of CaCO3 can come into being with the existence of HPMC. Meanwhile, the Mg2+ would inhibit the growth of calcite and facilitate the production of the aragonite when the Mg2+ concentration is lower than 25 mM in solution. With increasing the molar ratio of Mg/Ca, the nesquehonite precipitation would be induced when the magnesium concentration is sufficiently high. The nesquehonite grew along the same (4 0 0) orientation in that the HPMC can be controlled by the basic units during the aggregation and reorientation process. The results of polarizing microscope also provided forceful support for the crystal growth mechanism. The thermodynamical stable phase of anhydrous calcium carbonate (CaCO3) was nucleated preferentially after the combination between Ca2+ and CO32−, then, the Mg2+ can bond with the oxygen atoms in HPMC due to electrostatic adherence and combine with CO32− and H2O to form a nesquehonite crystal phase. The results illustrated that the extent of binding affinity during HPMC with Ca2+ or Mg2+ was suggested to be in connection with the reconstructuring process and the morphology of final carbonate crystals.

UNSUCCESSFUL DELIVERY OF TETRANDRINE FROM COLON-TARGETED DOSAGE FORMS COMPRISING ALGINATE/HYDROXYPROPYL METHYLCELLULOSE AND ALGINATE–CHITOSAN BEADS

Objective: The objective of this study was to optimize the formulations of antifibrotic tetrandrine beads using alginate and various concentrations ofhydroxypropyl methylcellulose (HPMC) and chitosan.Methods: Beads were formulated with six (F1–F6) concentrations of polymer and were then characterized using scanning electron microscopy,differential scanning calorimetry, and X-ray diffraction; these beads were used for measurements of moisture contents, swelling, and in vitro drugrelease.Results: Beads with the highest concentrations of HPMC and chitosan produced the highest entrapment efficiencies of 49.83% and 50.71%,respectively. Moreover, drug release under stomach conditions (HCl pH 1.2 medium) was restricted to 75.01%, 61.01%, 51.86%, 74.84%, 66.00%,and 41.63% with increasing HPMC and chitosan concentrations (F1–F6, respectively).Conclusion: Beads of all formulations showed inadequate retention of tetrandrine under pH conditions of the upper gastrointestinal tract and wouldlikely be unsuccessful as colon-targeted dosage forms.

Formulation and evaluation of transdermal drug delivery system of verapamil hydrochloride

The aim of this research was to develop and evaluate a matrix type of transdermal drug delivery system containing Verapamil Hydrochloride. The series of formulations containing Verapamil Hydrochloride were formulated by using different polymers like HPMC (hydrophilic), CAP (hydrophobic) and EC (hydrophobic) in different ratios by solvent evaporation technique. Propylene glycol and Dibutyl phthalate were used as plasticizers. The 20% and 40% of DMSO is used as the penetration enhancer. Formulated transdermal patches were physically evaluated for thickness, weight variation, drug content, flatness, tensile strength, folding endurance, and water vapour transmission rate. The in-vitro drug release study was carried out by using Franz diffusion cell. The data obtained from release study shows increased percentage of drug permeated in 20% of DMSO containing formulation than 40% of DMSO containing formulation. Drug permeation is enhanced in the formulation containing high concentration of HPMC (VH1). The VH2 and VH6 helped in maintaining the rate of release at a constant level (20% DMSO). But in case of 40% DMSO is used as the concentration of CAP increases the rate of permeation increases. Skin irritation study does not show any irritation on the skin of rabbit. There is no possible interaction between drug and polymers in FITR as well as DSC. XRD of selected formulation shows that drug present in the formulation is in crystalline form.&#x0D; Keywords: Verapamil HCl, HPMC, EC, CAP, DMSO, TDDS, Solvent evaporation

FORMULATION AND OPTIMIZATION OF FLOATING TABLETS OF CLOPIDOGREL BISULPHATE USING DESIGN OF EXPERIMENTS

Objective: The present study aimed at designing of floating matrix tablet of clopidogrel bisulphate by design of experiments.Methods: The tablets were prepared by direct compression technique using hydroxypropyl methylcellulose K15 (HPMC) as a matrix polymer and sodium bicarbonate as a gas generating agent. In order to optimize the concentration of HPMC (X1) and sodium bicarbonate (X2), a 32 full factorial design was employed. The tablet formulations were evaluated for floating lag time (Y1), floating or buoyancy time (Y2), percent water uptake, and differential scanning calorimetry (DSC) and in vitro drug release (Y3).Results: The formulation variables, HPMC concentration, and sodium bicarbonate concentration exerted a significant effect on floating behavior and drug release characteristics of the tablet. The optimized formulation, with 15% sodium bicarbonate concentration and 30 % HPMC concentration resulted in 5±2.6 sec of floating lag time, 22.0±0.6 h of floating time and 42.0±0.99% of clopidogrel bisulphate release in 8 h of dissolution study. The drug release mechanism was identified as nonfickian. The water uptake studies revealed that with an increase in HPMC concentration, there was an increase in swelling index of tablet whereas higher sodium bicarbonate concentration supported the faster erosion of matrix tablets. DSC study revealed no interaction of drug and polymers. The lower percentage error between predicted and observed responses of the optimized formulation validated the design.Conclusion: The study demonstrated successful designing of floating clopidogrel bisulphate tablet with factorial design.

Formulation and In vitro Evaluation of Unfolding Type Expandable Gastroretentive Film of Enalapril Maleate

The present work was based on the development and characterization of unfolding type gastroretentive dosage form appropriate for controlled release of enalapril maleate. Drug loaded films were prepared by solid dispersion technique using methocel K15 and eudragit RSPO and eudragit RLPO as polymers and polyethylene glycol 400 (PEG 400) as the plasticizer. The film folded in a capsule shell was shown to unfold in the gastric juice and provide drug release up to 12 h in the acidic medium. Formulations provided satisfactory unfolding characteristics allowing expansion to remain in the stomach. Formulation containing above 60% content of eudragit RSPO and eudgrait RLPO combination of total polymer content provided satisfactory film integrity over 12 hours. The result revealed that formulation F1 showed a minimum percentage of drug release of 63.41% followed by formulation F2, F3, F4 and F5 with 66.76%, 80.21%, 83.26% and 86.92% release in 8 hour respectively. Formulation with high proportion of eudragit RLPO and RSPO combination in total polymer content was found to be slow in drug release and lower the release from the polymeric film over time. As the concentration of HPMC K 15 in total polymer content increased the release rate of enalapril maleate as well as % release from the polymeric film also increased over time. Most of the formulation followed Higuchi release kinetics followed by Korsmeyer release kinetics. The drug release mechanism from the film follows Fickian and Non Fickian release kinetics. The films were evaluated for mechanical properties, in vitro drug release and unfolding behavior based on the mechanical shape memory of polymers. Absence of drug polymer interaction and uniform drug dispersion in the polymeric layers was revealed by DSC, FT-IR and SEM studies.Bangladesh Pharmaceutical Journal 20(2): 148-154, 2017

Formulation and evaluation of docetaxel nanosuspensions: In-vitro evaluation and cytotoxicity

ObjectiveThe aim of the present study was to formulate the anticancer drug; docetaxel (DOX) as nanoparticles to enhance its biological activity. MethodologySolvent precipitation method was used to prepare DOX-loaded nanoparticles and was stabilized by different concentrations of hydroxypropyl methylcellulose (HPMC, E5) and sodium deoxycholate (SDC). ResultsThe results showed that the particle size of the prepared DOX nanoparticles stabilized by SDC was small in comparison to those stabilized by the corresponding HPMC concentrations. The smallest particle size (83.97 nm) was obtained by using SDC as stabilizer at 5% level with zeta potential of −13.6 mV. It was concluded that increasing the stabilizer concentration resulted in increase in both initial and overall cumulative drug release. The release rate in case of nanoparticles stabilized by 5% SDC was 33% and 87% after 1 and 24 h respectively. The results showed that a significant reduction in the viability of FRO cells was observed at all tested time intervals in case of nanoparticles stabilized by 5% SDC at concentrations of 100 and 1000 μM/ml. In contrast, no signs of cytotoxicity was observed for nanoparticles stabilized by 5% HPMC at 10 and 100 μM/ml concentrations.

DEVELOPMENT AND EVALUATION OF CIPROFLOXACIN HYDROCHLORIDE LOADED OCULAR INSERT BY USING “PLANTAGO OVATA” AS NATURAL POLYMER

Objective: The present work focus in the direction of “Development and evaluation of Ciprofloxacin Hydrochloride loaded ocular insert by using “plantago ovata” as natural polymer”. The current work was carried out to evaluate the control release profile of ocular insert. Natural polymer in ocular insert was used for studying the long acting property. Natural polymer is also used to enhance the bioavailability of drug and reduce toxicity. It is also used to increase the duration of action of drug for prolongs action and gives better in vitro performance as compare than to the conventional ocular formulation.Methods: Solvent casting method was used in the formulation of Ciprofloxacin Hydrochloride loaded ocular inserts. Different ocular insert formulations of varying polymer concentration were prepared. Ocular insert formulation H-1 to H-3 was prepared by using different concentration of HPMC and formulation P-1 to P-4 was prepared by using different concentration of Plantago Ovata.Results: The ocular inserts formulation was within the acceptable limits. All the pre formulation parameters of polymers such as derived properties, compressibility index, Hausner’s ratio, viscosity, melting point, swelling ratio, loss on drying, PH of mucilage solution and pre formulation of active pharmaceutical ingredient such as estimation of drug by using UV spectroscopy, determination of melting point, solubility, partition coefficient and FTIR for compatibility study of drug and excipient were evaluation. FTIR analysis also confirmed no drug-excipient interaction.Conclusion: Prepared inserts in the present study were semitransparent. The mixing of the drug in to the polymer is uniform, due to this; the drug content of all formulation is good. Formulation P4 was selected because it showed better release profile, drug content and other physicochemical properties than other formulated batch when compare. All the prepared inserts showed in vitro drug release for the period of 4 h as compare to the marketed formulation. An in vitro drug release study revealed that ocular formulation gives a prolong action. The formulation was found to be long acting.