Ratio Of Hydroxypropyl Methylcellulose Research Articles

In Situ Gelling Behavior and Biopharmaceutical Characterization of Nano-Silver-Loaded Poloxamer Matrices Designed for Nasal Drug Delivery.

A combination of Poloxamer 407 (P407) and hydroxypropyl methylcellulose (HPMC) hydrosols is proposed as an in situ thermo-gelling vehicle for the nasal drug delivery of chlorhexidine-silver nanoparticles conjugates (SN-CX). Optimization of the formulation was carried out by applying varying ratios of P407 and HPMC in the presence and absence of SN-CX so that gelation would occur in the temperature range of the nasal cavity (30-34 °C). Mechanisms for the observed gelation phenomena were suggested based on viscosimetry, texture analysis, and dynamic light scattering. Tests were carried out for sprayability, washout time, in vitro drug release, ex vivo permeation, and antimicrobial activity. When applied separately, HPMC was found to lower the P407 gelation temperature (Tg), whereas SN-CX increased it. However, in the presence of HPMC, SN-CX interfered with the P407 micellar organization in a principally contrasting way while leading to an even further decrease in Tg. SN-CX-loaded nasal formulations composed of P407 16% and HPMC 0.1% demonstrated a desired gelation at 31.9 °C, good sprayability (52.95% coverage of the anterior nasal cavity), mucoadhesion for 70 min under simulated nasal clearance, expedient release and permeation, and preserved anti-infective activity against seasonal Influenza virus and beta-coronavirus, Pseudomonas aeruginosa, Klebsiella pneumoniae, Staphylococcus aureus and other pathogens. Our findings suggest that the current development could be considered a potential formulation of a protective nasal spray against respiratory infections.

Biological denitrification performance of a novel sulfur-slow-release carbon source mixed filler

Long-term operation of the sulfur autotrophic denitrification (SAD) process leads to pH reduction, nitrite accumulation, a low nitrogen removal efficiency and excessive sulfate in the effluent. Two slow-release carbon source (SRC) fillers (reactors S2 and S3) consisting of different ratios of hydroxypropyl methyl cellulose, disodium fumarate, polyhydroxy fatty acid ester and Fe3O4 powder were designed to couple SAD with heterotrophic denitrification by using SRC and sulfur particles (reactor S1) as components, combining the advantages of both processes while avoiding secondary pollution. During reactor operation, S3 showed the best denitrification performance. Under the optimal hydraulic retention time of 4 h, different influent nitrate concentrations of 39.92 ± 0.59 mg/L and 20.22 ± 0.45 mg/L achieved average nitrate removal efficiencies up to 88.01 ± 3.62 % and 94.28 ± 2.52 %, and the average denitrification strength were 8.78 mg N/(L·h) and 4.77 mg N/(L·h), respectively. 16S rRNA gene analysis at the genus level showed that the coupled reaction had the highest relative abundance of Thiobacillus associated with SAD, and SAD dominated the coupled system.

Active whey protein/hydroxypropyl methylcellulose edible films incorporated with cinnamaldehyde: Characterization, release kinetics and application to Mongolian cheese preservation

Edible films with modulated release of antimicrobial agents are important for food preservation. Herein, antimicrobial edible films were prepared using whey protein (WP) and hydroxypropyl methylcellulose (HM) as polymer matrix materials and cinnamaldehyde (CIN) as antimicrobial agent. The mass ratios of WP and HM were 100/0, 75/25, 50/50, 25/75 and 0/100. The release kinetics of CIN through the film was studied, applying the Fickian model, power law and Weibull model. The films were also characterized by physical and structural characteristics, and antibacterial activity. In comparison to other films, the CIN-loaded film with a WP/HM ratio of 50/50 had better moisture resistance, water vapor barrier properties and mechanical properties. High correlation factors were obtained by fitting the CIN release data with the power law (R2 > 0.96) and Weibull model (R2 > 0.97). The diffusion mechanism of CIN was pseudo-Fickian. The diffusion coefficients (D1 and D2) had a positive linear relationship with the HM ratio, suggesting that a high HM ratio was beneficial to the CIN release. Finally, the WH50-C film was successfully used to preserve Mongolian cheese. This research provides a new perspective on the design of active packaging film with sustained-release characteristics.

Solution blow spun flexible zirconia nanofibers toward high-performance 2D and 3D nanostructures

Polymer templates are critical in the preparation of ceramic fibers from precursor solutions, but the available options are limited. Here, ZrO2 nanofiber films and aerogels are developed by solution blow spinning method using hydroxypropyl methylcellulose (HPMC) and polyvinylpyrrolidone (PVP) as templates. The effects of HPMC ratio, polymer concentration, and calcination temperature on the morphology and structure of the ZrO2 nanofibers are investigated. The nanofiber films with an areal density of 20 mg cm−2 exhibit excellent filtration property, achieving a filtration efficiency of 94.94% and a pressure drop of 136 Pa at an airflow velocity of 32 L min−1. The nanofiber aerogels display low density of 50 mg cm−3, low thermal conductivity of 0.039 W m−1 K−1, as well as superior compressibility, demonstrating significant potential for thermal protection applications. This work expands the formation template option of ceramic fibers, offering significant guidance in the development of flexible, high-temperature-resistant ceramic fiber materials.

Formulation and characterization: Metoprolol succinate controlled release matrix tablets

Metoprolol succinate-controlled release matrix tablets were made utilizing the wet granulation process with various ratio of Hydroxypropyl methyl cellulose (HPMC K4M). Isopropyl alcohol is used as a granulating agent in the Povidone (PVP K30) solution. In addition to being utilised as diluents to raise the weight of the tablets, magnesium stearate and talc were added to enhance the granules' flow ability during tablet compression. The crushed tablets underwent physicochemical characteristics, in-vitro and kinetic tests, and the micromeritic properties of the generated granules were evaluated. In every formulation, results were nearly satisfactory, with M4 being the best among the others. All of the formulations showed good correlation. The drug diffusion kinetics from matrix tablets appeared to be zero order, and the release mechanism was diffusion regulated.

Development of Face Pack Powder of Arabica Coffee (Coffea arabica L.) Using Variations of Binders with D-Optimal Mixture Design

Cosmetics like face pack powder are popular preparations used by men and women. Hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (CMC-Na) and carbopol are commonly used binders and are suited to dispersal by water. Many natural ingredients such as arabica coffee (Coffea arabica L.) are useful for cosmetics. Chlorogenic acid and α-tocopherol is a bioactive compound for antioxidant activity and is important in its application in face pack powder. This study aimed to determine the ratio comparison of the composition of the three polymers used as the binders for preparations of the coffee face pack powder using a D-optimal mixture design, analyze the evaluation results of the optimum face pack powder formula, and determine its antioxidant activity. The study began with coffee extraction with 70% ethanol as solvent, wet granulation process with binders and other excipients, evaluation of organoleptic properties, pH, and water content, stability observation for 28 days, and in-vitro measurement of antioxidant activity. One-sample t-test was applied to analyze the results. The obtained optimum formula was with the ratio of HPMC (8.43): carbopol (1.16): CMC-Na (5.41). The evaluation results of the optimum formula showed that the face pack powder has ash brown color, weak aromatic typical coffee fragrance, homogeneous texture, pH value of 5.93 ± 0.06, and water content of 0.89 ± 0.15%. The resulting study shows the coffee face pack powder and crude extract have antioxidant activity (34.94 ppm ± 0.75 and 15.78 ppm ± 2.53). The analysis with the one-sample t-test showed that the experimental results were not significantly different from the software predictions, so the Design-Expert® software using the D-optimal mixture design is applicable to predict the optimum formula of coffee face pack powder

Effect of cellulose derivatives on the morphology, agglomeration, and phase transformation of spinel nanoparticles prepared via modified sol-gel method and comparison of optical transmission of spark plasma sintered ceramic

The Pechini method is one of the alkoxide sol–gel methods in which citric acid (CA) and ethylene glycol (EG) pair are used for gel preparation. The major downside of this method is an agglomeration of the produced nanoparticles. In this research, by substituting ethylene glycol chelating agent with cellulose derivatives (such as carboxy methyl cellulose (CMC) and hydroxy propyl methyl cellulose (HPMC), the reduction of the extent of spinel nanoparticle agglomeration is examined. To this aim, a different ratio of CMC and HPMC to metal ions (Mg2+ and Al3+) was used. The results indicated that the sample synthesized with 1 g CMC had the minimum agglomeration and particle size (50 nm). Next, this sample was consolidated through the spark plasma sintering method at 1500 °C for 15 min. The microstructure, grain size and optical transmittance of the SPSed body were compared with the sample prepared with the conventional Pechni method. The results showed that the maximum visible light and infrared transmission of the bulk prepared from the modified Pechini method was higher than that of the sample prepared via the conventional Pechini method. The optimal visible light transmission was 85%, and in the IR region at a wavelength of 5 µm was 75%. This is related to the higher apparent density of this ceramic (99.98% vs 98.82%) and the lower porosity of this sample.

The effect of polymeric films of hydroxypropyl methylcellulose (HPMC)/chitosan on ofloxacin release, diffusion, and biological activity

AbstractInfectious diseases caused by resistant bacteria have been investigated by several researchers recently. Ofloxacin is a quinolone antibiotic used against resistant microorganisms and in different routes of administration. Transdermal drug delivery is used to reduce drug toxicity, avoid first‐pass metabolism, and reduce fluctuations in drug concentration in the body. Ofloxacin was formulated in a transdermal polymeric formula using hydroxypropyl methyl cellulose (HPMC) and chitosan at different ratios in the presence of palmitic acid as a permeation enhancer. Physical characterization, drug release and diffusion, drug matrix association, and antimicrobial assay have been investigated using different techniques including HPLC, fourier‐transform infrared spectroscopy (FTIR), Franz cells diffusion, and UV spectroscopy. Ofloxacin release was successfully accomplished in many polymeric formulas containing a high ratio of HPMC with a maximum drug release of 53%. Formulas selected for antimicrobial assay indicate that sustained release patches have successfully inhibited microbial and biofilm growth with a percentage inhibition of more than 90%. In conclusion, antibiotics can be formulated in transdermal polymeric film to target skin infection and reduce drug toxicity and avoid drug first metabolism for drugs reaching systemic circulation which has a direct influence on drug activity.

Enhancing the Dissolution of Oral Dasatinib Tablets Using Zein–Hydroxypropyl Methylcellulose Solid Dispersions

Zein has been used in several pharmaceutical applications because of its unique composition. It is an amphiphilic molecule that is biodegradable, biocompatible, and has adhesive, matrix-forming, and film-coating properties, making it a promising pharmaceutical excipient. Zein-based formulations have been investigated in tablet-coating, nanoparticulate delivery systems, and controlled-release formulations. However, to date, very few studies have been performed on the inclusion of zein in solid dispersion formulations to enhance drug dissolution. This study aimed to improve the dissolution of the weakly basic and poorly soluble oral dasatinib (used as a model) using zein–hydroxypropyl methylcellulose (HPMC) solid dispersion to achieve rapid disintegration and dissolution in the gastric pH. Using the spray-drying technique, four solid dispersions were prepared with different zein, HPMC, and dasatinib ratios. Subsequently, five different tablets were directly compressed using the previously prepared solid dispersions along with basic excipients. Various in vitro characterization analyses were performed to predict their behavior in vivo. Particle size measurement, tablet weight variation and content assay, disintegration, and dissolution studies were also performed. The results indicated that zein solid dispersion improved the disintegration and dissolution of dasatinib in the gastric media by reducing the drug particle size and the formation of the dasatinib amorphous state. Moreover, the tablets exhibited desirable properties in terms of high drug content, friability, and tensile strength. In conclusion, tablets comprising zein–HPMC solid dispersion showed improved properties; however, including a higher ratio of zein in the solid dispersion adversely affected the disintegration and release properties of formulations.

Formulation and Evaluation of Hydroxypropylmethylcellulose-dicyclomine Microsponges for Colon Targeted Drug Delivery: In Vitro and In Vivo Evaluation.

The objective of the present study was to design novel colon targeted delivery of Dicyclomine Hydrochloride (DCH) microsponges. Microsponges (MS1-MS4) based on different ratios of Hydroxypropylmethylcellulose (HPMC) and DCH were prepared by quasi-emulsion solvent diffusion method. Micro-sponges were analyzed by determining percent yield, encapsulation efficiency, drug content, drug-polymer compatibility and thermal stability. Kinetic analysis of thermal stability data was done by Chang method, Friedman method and Broido method. In vitro dissolution study was carried out at pH 1.2, pH 6.8 and pH 7.4 at different time intervals. Results showed that there was no chemical interaction between DCH and HPMC in all microsponge formulations. Production yield, drug content and encapsulation efficiency were enhanced on increasing the drug-polymer ratio. Thermal stability of all the micro-sponges was greater than that of pure drug. In vitro drug release was decreased on increasing the polymer concentration at different pH levels. The newly prepared micro-sponges based on HPMC were confirmed as a promising means of colon-targeted delivery of DCH. An HPLC method was developed and validated for the bioequivalence study of newly designed microsponges. Pharmacokinetics parameters were calculated using the linear trapezoidal method after single oral administration of microsponges in white albino rabbits. Pharmacokinetics results indicate an enhancement in the value of t1/2, tmax, Cmax and AUC0-t of DCH in the microsponges as compared to standard DCH showing enhanced bioavailability of the drug after microsponges formation. The current study shows a new approach for colon-specific delivery of DCH based on microsponges.

Hybridization of glucosyl stevioside and hydroxypropyl methylcellulose to improve the solubility of lutein

In this paper, a lutein-glucosyl stevioside (stevia-G)-hydroxypropyl methylcellulose (HPMC) complex was prepared via an antisolvent precipitation combined with dynamic high pressure microfluidization method. The solubility, microstructure, crystallinity and thermodynamic properties of the freeze-dried powder were investigated, as well as the formation mechanism and the storage stability of the produced complex. When the optimal mass ratio of lutein, stevia-G, and HPMC was 1: 40: 0.5, the apparent solubility of lutein reached 2805.47 ± 24.94 μg·mL−1, which was approximately 5600 times higher than that of lutein crystals. The lutein-stevia-G-HPMC complex formed an amorphous dispersed structure and was in a thermodynamically high energy state. The self-assembled micelle structure of stevia-G and HPMC polymer created a supersaturated system mainly by multiple hydrogen bonding, which promoted maximum lutein dissolving, delayed supersaturated crystallization process, and hindered precipitation. The present results suggested the complex formed by stevia-G and HPMC effectively promote lutein’s hydrophilicity and stability.

Solid Dispersion of Tenoxicam – HPMC by Freeze-Drying: Solid State Properties, Dissolution Study, and Analgesic Activity in Mice

AIM: The aim of this study was to prepare solid dispersion of tenoxicam with hydroxypropyl methylcellulose (HPMC) to improve solubility, dissolution rate, and in vivo analgesic activity. METHODS: Solid dispersion of tenoxicam with HPMC was prepared using the freeze-drying technique in three ratios of drug to carrier (1:1, 1:2, and 2:1 w/w). The s olid-state properties of solid dispersion powders were characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR) spectroscopy, and scanning electron microscope (SEM). Solubility and dissolution rate studies were conducted in an aqueous medium. Analgesic activity was evaluated using the writhing method. RESULTS: Analysis of PXRD and DSC results indicated a decreased degree of crystallinity of tenoxicam in solid dispersion powders. Solid dispersion of tenoxicam exhibited a significant improvement in solubility and dissolution rate compared to intact tenoxicam, in line to the increment on the ratio of HPMC. Analgesic activity study revealed that solid dispersion 1:2 was more effective than intact tenoxicam. CONCLUSIONS: This study concludes that the solid dispersion technique is a promising strategy to improve the solubility and dissolution rate of tenoxicam.

Impacts of addition ratio of hydroxypropyl methyl cellulose or guar gum on the quality of high fiber pasta from wheat flour and mung bean husk

The production of dehulled mung bean seed generates the husk which is currently used in the manufacturing of animal feed. This by-product is rich in dietary fiber and can be used as a dietary fiber source for supplementation to food products. The pasta originated from 85% wheat flour and 15% by-product of dehulled mung bean seed production had high dietary fiber content and met the requirement of a high fiber food. Nevertheless, the use of mung bean husk negatively affected cooking properties, textural profile and sensorial quality of high fiber pasta. In this study, the effects of addition ratio of hydroxypropyl methyl cellulose (HPMC) and guar gum (GG) on the quality of pasta originated from 85% wheat flour and 15% mung bean husk were investigated. Increase in HPMC or GG ratio from 0 to 2% gradually decreased the cooking loss while improved the optimal cooking time, water absorption index, adhesiveness, cohesiveness, elongation rate as well as the overall acceptability of high fiber pasta. The increased hardness of the product added with HPMC was recorded while this property was reduced when GG was used in the pasta formulation. The use of HPMC resulted in pasta sample with better textural profile and overall acceptance than that of GG.

Chlorhexidine Mucoadhesive Buccal Tablets: The Impact of Formulation Design on Drug Delivery and Release Kinetics Using Conventional and Novel Dissolution Methods.

Oropharyngeal candidiasis (OPC) is a mucosal infection caused by Candida spp., and it is common among the immunocompromised. This condition is mainly treated using oral antifungals. Chlorhexidine (CHD) is a fungicidal and is available as a mouth wash and oral gel. It is used as an adjuvant in the treatment of OPC due to the low residence time of the current formulations. In this study, its activity was tested against C. albicans biofilm and biocompatibility with the HEK293 human cell line. Then, it was formulated as mucoadhesive hydrogel buccal tablets to extend its activity. Different ratios of hydroxypropyl methylcellulose (HPMC), poloxamer 407 (P407), and three different types of polyols were used to prepare the tablets, which were then investigated for their physicochemical properties, ex vivo mucoadhesion, drug release profiles, and the kinetics of drug release. The release was performed using Apparatus I and a controlled flow rate (CFR) method. The results show that CHD is biocompatible and effective against Candida biofilm at a concentration of 20 µg/mL. No drug excipient interaction was observed through differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR). The increase in P407 and polyol ratios showed a decrease in the swelling index and an increase in CHD in vitro release. The release of CHD from the selected formulations was 86–92%. The results suggest that chlorhexidine tablets are a possible candidate for the treatment of oropharyngeal candidiasis.

It is Possible to Achieve Tablets With Good Tabletability From Solid Dispersions - The Case of the High Dose Drug Gemfibrozil.

Solid Dispersions (SDs) have been extensively used to increase the dissolution of poorly water-soluble drugs. However, there are few studies exploring SDs properties that must be considered during tablet development, like tabletability. Poorly water-soluble drugs with poor compression properties and high therapeutic doses, like gemfibrozil, are an additional challenge in the production of SDs-based tablets. This study evaluates the applicability of SDs to improve both tabletability and dissolution rate of gemfibrozil. A SD-based tablet formulation was also proposed. SDs were prepared by ball milling, using hydroxypropyl methylcellulose (HPMC) as a carrier, according to a 23 factorial design. The formulation variables were gemfibrozil:HPMC ratio, milling speed, and milling time. The response in the factorial analysis was the tensile strength of the compacted SDs. Dissolution rate and solid-state characterization of SDs were also performed. SDs showed simultaneous drug dissolution enhancement and improved tabletability when compared to corresponding physical mixtures and gemfibrozil. The main variable influencing drug dissolution and tabletability was the gemfibrozil:HPMC ratio. Tablets containing gemfibrozil- HPMC-SD (1:0.250 w/w) and croscarmellose sodium showed fast and complete drug release, while those containing the same SD and sodium starch glycolate exhibited poor drug release due to their prolonged disintegration time. SDs proved to be effective for simultaneously improving tabletability and dissolution profile of gemfibrozil. Tablets containing gemfibrozil-HPMC-SD and croscarmellose sodium as disintegrating agent showed improved drug release and good mechanical strength, demonstrating the potential of HPMC-based SDs to simultaneously overcome the poor dissolution and tabletability properties of this drug.

Optimization of Hydroxypropyl Methylcellulose and Dextrin in Development of Dried Nanosuspension for Poorly Water-Soluble Drug.

The purpose of this study is to identify the effects of a stabilizer and matrix former in the development of a celecoxib dried nanosuspension (DNS) for high dissolution rate and drug loading. Tween 80 and Hydroxypropyl Methylcellulose (HPMC) were used as stabilizers in the bead-milling process and dextrin was used as the matrix former in the spray-drying. Various nanosuspensions (NS) were prepared by varying the ratio of HPMC and dextrin, and the physicochemical properties of each formulation were evaluated for particle size, morphology, drug loading, crystallinity, redispersibility, physical stability and dissolution rate. HPMC efficiently stabilized the NS system and reduced the particle size of NS. The mean particle size of the NS with 0.5% HPMC (w/v) was the smallest (248 nm) of all formulations. Dextrin has been shown to inhibit the increase of particle size efficiently, which is known to occur frequently when NS is being solidified. As the dextrin increased in DNS, the dissolution rates of reconstituted NS were significantly improved. However, it was confirmed that more than the necessary amount of dextrin in DNS reduced the dissolution and drug loading. The dissolution of celecoxib in DNS prepared at the ratio (drug:dextrin, 1:2.5) was almost the highest. The dissolution of optimal formulation was 95.8% at 120 min, which was 2.0-fold higher than that of NS dried without dextrin. In conclusion, these results suggest that the formulation based on Tween 80, HPMC and dextrin may be an effective option for DNS to enhance its in vitro dissolution and in vivo oral absorption.

The Effect of Combination of Hydroxypropylmethylcellulose and Carboxymethylcellulose Sodium Polymers to The Physical Properties of Celery (Apium graveolens L.) Ethanolic Extract Patch

Celery herbs (Apium graveolens L.) contain apigenin compounds (flavonoids) that are effective as antihypertensiv. Celery herbs used in the form of decoction and oral preparations have a deficiency that is voluminous and can cause gastric irritation. Patches were chosen because it can prevent gastric irritation and reduce the frequency of drug administration because the drug is delivered over the skin with a long duration. This study aimed to know the effect of variations in the ratio of the concentrations of hydroxypropyl methylcellulose (HPMC) and carboxymethylcellulose sodium (CMC sodium) polymers to the physical properties of celery herbs ethanol extract patch.This study was conducted with maceration of celery herbs using 96% ethanol and then dispersed in patch made with variations in the concentrations ratio of HPMC and CMC sodium polymers of 3:1, 1:1, and 1:3. Patches were tested for physical properties including organoleptic, pH, thickness, weight, folding endurance, and moisture content. Statistical analysis of test data used One Way ANOVA and Paired Samples T Test.The results of statistical analysis showed that the increase concentrations ratio of CMC sodium polymer in the combination of HPMC and CMC sodium polymers could increase the thickness, weight, and moisture content of celery herbs ethanol extract patch. The best patch was formula 2 with the same concentration ratio of HPMC and CMC sodium polymers because it showed the best results with a pH 6,12-6,29, thickness 1,37-1,53 mm, weighting 2,24-2,52 gram, folding endurance more than 300 times, and the moisture content was quite stable.

Chemical mapping analysis of compatibility in gelatin and hydroxypropyl methylcellulose blend films

Blending different polymers for composite formulations can improve the functionalities of the products. The compatibility between hydroxypropyl methylcellulose (HPMC) and gelatin was studied using Chemical mapping analysis such as synchrotron micro-infrared spectroscopy (μSR-FTIR) and confocal Raman microscopy. The interface and phase composition of the blend films with varying ratios of gelatin and HPMC were analyzed in detail. It was found that the distribution patterns of continuous matrices and dispersed phases changed with varying concentrations of the components. Raman spectroscopy based imaging analysis showed that HPMC easily aggregated to form continuous phases. Both μSR-FTIR and Raman microscopic analysis confirmed the existence of intermediate phases in the composites from the molecular interactions between the two components. Overall, the Chemical mapping techniques were useful to study the phase composition of composites of polysaccharides and proteins.

Fast Dissolving Sublingual Strips: A Novel Approach for the Delivery of Isosorbide Dinitrate

Background: Isosorbide dinitrate (ISDN) is used for treating the angina attacks. In addition, oral ISDN is available in immediate and sustained release formulations and the bioavailability of ISDN is about 20-25% when taken orally. Further, the ISDN films are developed for sublingual drug delivery by improving drug bioavailability. The present study aimed to design and evaluate the physicochemical properties of the film formulation for sublingual delivery of ISDN. Methods: In the present study, sublingual films were prepared by the solvent casting technique using the hydroxypropyl methylcellulose (HPMC) polymers (i.e., 100, 150 and 200 mg) with a different drug to polymer ratios (i.e., 1:5, 1:7.5 and 1:10). Then, ISDN was evaluated for the film appearance, drug content, surface pH, mucoadhesion force, differential scanning calorimetry (DSC), in vitro drug release, and ex vivo permeability. Results: Based on the results, F3 formulation (1:10 ISDN to HPMC ratio) showed acceptable thickness (0.93 mm), weight (11.14 mg), surface pH (7.82), moisture absorption capacity (6.08%), elasticity (>200), mucoadhesion force (18.05 N/cm2), and drug content (6.22%). Furthermore, the results demonstrated that HPMC polymer improved the characteristics of the films, modified the bioadhesiveness, and finally, enhanced elasticity. However, DSC thermogram failed to show any crystalline drug substance in the films except for F1 (immediate release) and the endothermic peak of ISDN was absent in F2 and F3 films. Therefore, the drug which was entrapped into the film was in an amorphous or disturbed-crystalline phase of the molecular dispersion or dissolved in the melted polymer in the polymeric matrix. Moreover, the drug release from the films was faster compared to the tablet® (P<0.05). Conclusion: In general, the formulation of F1 was observed to be an appropriate candidate for developing the sublingual film for the remedial use.

Effects of some process parameters on the niflumic acid controlled release polymeric microspheres: Optimization using designs of experiments

AbstractMicroparticles charged by niflumic acid and based on cellulose derivatives as polymeric matrices, that is, ethylcellulose (EC) and mixtures of EC and hydroxypropylmethylcellulose (HPMC), were elaborated using microencapsulation by emulsion‐solvent evaporation technique. The niflumic acid is considered as a poorly water soluble drug, so the main objective of the paper is to use designs of experiment in order to prepare new solid formulations with a large range of size for the drug dissolution enhancement. The possible drug–polymer interaction was investigated by Fourier transform‐infrared spectroscopy, X‐ray diffraction, and differential scanning calorimetric analysis. Some of the process variables, namely, the stirring speed of emulsion, the emulsifier concentration, and the EC:HPMC ratio, were selected and varied. Their main and interactive effects on the microparticles' characteristics were obviously evaluated and discussed using Minitab software 16.1. The obtained microparticles' size (d10) ranged from 196 to 796 μm, and the drug entrapment reached 45% in some formulations. The drug dissolution results showed that the Higuchi's release constant varied from 0.011 to 0.067 min−1/2 and was enhanced especially when the HPMC concentration was increased.