Propose: Bacterial pneumonia is a common lung infection caused by different types of bacteria. Azithromycin (AZI), an azalide antibiotic, is widely used to manage pneumococcal infections. Studies have shown that antibiotics in nanocarriers may lead to increased antibacterial activity and reduced toxicity. The aim of this work was to valuate in vitro antibacterial performance azithromycin-EUDRAGIT RS100 nano-formulations against Streptococcus pneumoniae and Staphylococcus aureus.Methods: AZI-EUDRAGIT RS100 nanoparticles were prepared via electrospinning technique and the in vitro antibacterial performance against S. pneumoniae and S. aureus were assessed using agar dilution method.Results: Nanofibers in the sizes about 100-300 nm in diameter and micro scale in length and nanobeads in the range of 100-500 nm were achieved. The Minimum Inhibitory Concentrations (MIC) showed an enhancement in the antimicrobial effect of AZI-EUDRAGIT RS100 nanofibers (40 mg/ml) compare to untreated AZI solution (>160 mg/ml) against S. pneumonia. The MIC value for AZI-EUDRAGIT RS100 nanofibers against S. aureus was>128 mg/ml, same as that of the untreated AZI solution.Conclusion: The enhanced efficiency of AZI in nanofibers could be related to the more adsorption opportunity of nanofibers to S. pneumonia capsulated cell wall which provides an antibiotic depot on the bacterial surface compared to S. aureus. AZI-EUDRAGIT RS100 nanofibers with enhanced antimicrobial effect against S. pneumonia can be considered as a candidate for in vivo evaluations in antibiotic therapy of Pneumococcal infections.

A sustained-release tablet formulation should ideally have a proper release profile insensitive to moderate changes in tablet hardness that is usually encountered in manufacturing. In this study, matrix aspirin (acetylsalicylic acid) tablets with ethylcellulose (EC), EUDRAGIT RS100 (RS), and EUDRAGIT S100 (S) were prepared by direct compression. The release behaviors were then studied in two counterpart series of tablets with hardness difference of three Kp units, and compared by non-linear regression analysis. The release pattern for both the S-containing and RS-containing formulations fitted best in Higuchi model, and the proper equations were suggested. In the EC-containing formulation, Higuchi and also zero-order models were probable models for the release, and a combination equation for the release was suggested. In the S-containing formulation, the release profile was completely sensitive to the hardness change. In RS-containing series, the slope of the release graph did not change due to the hardness decrease, but the y-intercept or the lag time in release was decreased. In EC-containing matrix tablets, both the slopes and the y-intercepts did not change by the decrease in hardness. In conclusion, EC with an amount as little as 10 percent in formulation could make sustained-release aspirin tablets in which the release profile is not sensitive to moderate changes in hardness.

Purpose: Echinacea purpurea (L. ) Moench is a member of the Asteraceae family and is traditionally used mainly due to its immunostimulatory properties. Various compounds including alkylamides and chicoric acid were reported as active ingredients of E. purpurea. Here, we aimed to prepare electrosprayed nanoparticles (NPs) containing hydroalcoholic extract of E. purpurea using EUDRAGIT RS100 (EP-EUDRAGIT RS100 NPs) to improve the immunomodulatory effects of the extract. Methods: The EP-EUDRAGIT RS100 NPs with the different extract: polymer ratios and solution concentrations were prepared using the electrospray technique. The size and morphology of the NPs were evaluated using dynamic light scattering (DLS) and field emission-scanning electron microscopy (FE-SEM). To evaluate the immune responses, male Wistar rats were administrated with the prepared EP-EUDRAGIT RS100 NPs and plain extract in the final dose of 30 or 100 mg/kg. The blood samples of the animals were collected and the inflammatory factors and complete blood count (CBC) were investigated. Results: In vivo studies indicated that the plain extract and EP-EUDRAGIT RS100 NPs (100 mg/kg) significantly increased the serum level of tumor necrosis factor-α,(TNF-α, ) and interleukin 1-β,(IL1-β, ) whereas the EP-EUDRAGIT RS100 NPs (30 mg/kg) significantly increased the number of white blood cells (WBCs) compared to the control group. Lymphocytes’,count in all groups was increased significantly compared to the control group (P < 0. 05) whereas other CBC parameters remained unchanged. Conclusion: The prepared EP-EUDRAGIT RS100 NPs by electrospray technique caused significant reinforcement in the immunostimulatory effects of the extract of E. purpurea.

Purpose: The purpose of this work was to preparation of vancomycin (VCM) biodegradable nanoparticles to improve the intestinal permeability, using water-in-oil-in-water (W/O/W) multiple emulsion method.Methods: The vancomycin-loaded nanoparticles were created using double-emulsion solvent evaporation method. Using EUDRAGIT RS100 as a coating material. The prepared nanoparticles were identifyed for their micromeritic and crystallographic properties, drug loading, particle size, drug release, Zeta potential, effective permeability (Peff) and oral fractional absorption. Intestinal permeability of VCM nanoparticles was figured out, in different concentrations using SPIP technique in rats.Results: Particle sizes were between 362 and 499 nm for different compositions of VCM-RS-100 nanoparticles. Entrapment efficiency expansed between 63%-94.76%. The highest entrapment efficiency 94.76% was obtained when the ratio of drug to polymer was 1: 3. The in vitro release studies were accomplished in pH 7.4. The results showed that physicochemical properties were impressed by drug to polymer ratio. The FT-IR, XRPD and DSC results ruled out any chemical interaction betweenthe drug and RS-100. Effective intestinal permeability values of VCM nanoparticles in concentrations of 200, 300 and 400 mg/ml were higher than that of solutions at the same concentrations. Oral fractional absorption was achieved between 0.419-0.767.Conclusion: Our findings suggest that RS-100 nanoparticles could provide a delivery system for VCM, with enhanced intestinal permeability.

The drug-in-adhesive (DIA)-type matrix patches of lamotrigine are developed using variable permeation enhancers (oleic acid, PG, lemon oil and aloe vera), and drug in vitro release and its permeation are evaluated. Lamotrigine has been long used as an anti-epileptic, mood stabilizer, to treat bipolar disorder in adults and off label as an antidepressant. lamotrigine matrix patches comprising of EUDRAGIT ® RS100 (rate-controlling polymer) and DuroTak ® 387-2510 (adhesive) were prepared by pouring the solution on backing membrane (3M-9720). The thickness of 120 μ m was adjusted through micrometer film applicator. USP Apparatus V was used for the evaluation of release profile, which was fitted into various mathematical models. Quality characteristics of patches were determined through weight variation, moisture content, moisture uptake and drug content evaluation. FTIR studies were performed for drug-excipient compatibility; Franz diffusion cell was employed for studying in vitro permeation parameters such as flux, lag time, and ER. Skin sensitivity study of optimized patch was also performed. The release from patches comprising of PG and oleic acid was maximum, i. e., 96. 24 ± 1. 15% and 91. 12 ± 1. 11%, respectively. Formulations (A1– A5) exhibited Makoid– Banakar release profile. Formulation A3 consisting of oleic acid was optimized due to enhanced permeation of drug across skin compared to other enhancers with enhancement ratio of 3. 55. Skin sensitivity study revealed patch as safe and non-allergenic. The study demonstrates that oleic acid can be used as a suitable permeation enhancer for transdermal delivery of lamotrigine from matrix-type patches.

Ocular inserts of ofloxacin were prepared with objectives of reducing the frequency of administration, obtaining controlled release and greater therapeutic efficacy in the treatment of eye infections such as conjunctivitis, keratitis, corneal ulcers, etc. Polyvinyl alcohol (PVA) ofloxacin films were prepared by mercury substrate method. The ocular inserts were evaluated for drug-excipient interaction, physico-chemical characteristics, microbiological and in vitro and in vivo release studies. There was no interaction between drug and excipients as revealed by UV absorption and IR spectra of the pure drug, medicated and placebo formulations. The weight and thickness of the inserts were in the range of 57.3-126.0 mg and 55.6-99.3 microns, respectively for different formulations; casting of rate-controlling membrane increased the weight and thickness of the inserts. Tensile strength and percent elongation at break varied with the nature of rate-controlling membrane and film thickness. Moisture vapour transmission through films followed zero-order kinetics and decreased with increase in film thickness. The drug content varied from 99.53-99.86%. The method of exposure to UV radiation was used for sterilization of ocular inserts and no microbial growth was observed in any formulation during sterility testing by direct inoculation method. The influence of rate-controlling membrane of different polymers of ethyl cellulose (EC) and polymethacrylates (EUDRAGIT RL100, EUDRAGIT RS100) on release kinetics was studied. The drug release for prepared formulations with rate-controlling membrane of EC, EUDRAGIT RS100 (ERS), EUDRAGIT RL 100 (ERL) was found to be 85.80, 93.85 and 98.71%, respectively and followed zero-order kinetics. Ocular insert F3 with rate-controlling membrane of EUDRAGIT RS100, when inserted into the eye of rabbit showed controlled release up to 24 hours. There was a good correlation between in vitro and in vivo release data. The developed formulation was effective against selected microorganism during in vitro antimicrobial efficacy studies. PVA-ofloxacin ocular inserts with rate-controlling membrane of EUDRAGIT RS100 are promising for controlled ocular delivery of ofloxacin.

EUDRAGITs are synthetic copolymers of acrylate that have been known as suitable carriers for preparation of sustained release matrices. Solid dispersion (SD) systems which at first had been used to enhance the dissolution rate of poorly water soluble drugs is now widely used in preparation of sustained release matrices. This study was performed in order to evaluate the EUDRAGIT RL and RS solid dispersion systems in preparation of sustained release diclofenac sodium matrices. The effect of drug and polymer mixture preparation and drug polymer ratio on the properties of matrices such as its crushing strength, drug release rate and mechanism were studied. The results showed that increasing the polymer content increased the cl1lshing strength of matrices prepared either from physical mixture or SD system and decreased the rate of drug released. Matrices prepared from SD system were harder than those prepared from physical mixtures and the rate of drug release from former matrices was considerably slower than the latter matrices. Comparison of drug release at the same drug: polymer ratio showed that drug release rate from E.RL matrices was slower than E.RS matrices except in matrices prepared from physical mixture with I: 1 drug: polymer ratio. This was attributed to the electrostatic interaction between polymers and drug. The electrostatic interaction between drug and polymers was confirmed by measuring the amount of drug absorbed on the polymers in the presence of Tween 80 or SLS. As E.RL contains more ammonium groups than E.RS therefore the extent of interaction between dic10fenac sodium and E.RL could be greater than E.RS. This could explain the slower drug release rate from E.RL matrices compared to E.RS. In SD systems the extent of interaction between drug and polymers increased and this retarded the rate of drug released. It was shown that in the most cases diffusion was the main mechanism controlling drug release rate. In conclusion the use of solid dispersion systems is valuble in production of sustained release matrices of E.RL and E.RS and can lead to less polymer consumption compared to physical mixtures of drug and polymer in order to control drug release rate. These systems due to very slow rate of drug release are also useful in production of transdermal drug delivery systems.

A Box-Behnken design with three replicates was used for preparation and evaluation of EUDRAGIT vancomycin (VCM) nanoparticles prepared by double emulsion. The purpose of this work was to optimize VCM nanoparticles to improve the physicochemical properties. Nanoparticles were formed by using W1/O/W2 double-emulsion solvent evaporation method using EUDRAGIT RS as a retardant material. Full factorial design was employed to study the effect of independent variables, RPM (X1), amount of emulsifier (X2), stirring rate (X3), volume of organic phase (X4) and volume of aqueous phase (X5), on the dependent variables as production yield, encapsulation efficiency and particle size. The optimum condition for VCM nanoparticles preparation was 1: 2 drug to polymer ratio, 0.2 (%w/w) amount of emulsifier, 25 mL (volume of organic phase), 25 mL (volume of aqueous phase), 3 min (time of stirring) and 26000 RPM. RPM and emulsifier concentrations were the effective factors on the drug loading (R2=90.82). The highest entrapment efficiency was obtained when the ratio of drug to polymer was 1: 3. Zeta (z) potential of the nanoparticles was fairly positive in molecular level. In vitro release study showed two phases: an initial burst for 0.5 h followed by a very slow release pattern during a period of 24 h. The release of VCM was influenced by the drug to polymer ratio and particle size and was found to be diffusion controlled. The best-fit release kinetic was achieved with Peppas model. In conclusion, the VCM nanoparticle preparations showed optimize formulation, which can be useful for oral administrations.