Eudragit RS30D Research Articles

Thymol-Loaded Eudragit RS30D Cationic Nanoparticles-Based Hydrogels for Topical Application in Wounds: In Vitro and In Vivo Evaluation

Natural medicines formulated using nanotechnology-based systems are a rich source of new wound-treating therapeutics. This study aims to develop thymol-loaded cationic polymeric nanoparticles (CPNPs) to enhance the skin retention and wound healing efficacy of thymol. The developed materials exhibited entrapment efficiencies of 56.58 to 68.97%, particle sizes of 36.30 to 99.41 nm, and positively charged zeta potential. In Vitro sustained release of thymol up to 24 h was achieved. Selected thymol CPNPs (F5 and C2) were mixed with methylcellulose to form hydrogels (GF5 and GC2). An In Vivo skin-retention study revealed that GF5 and GC2 showed 3.3- and 3.6-fold higher retention than free thymol, respectively. An In Vitro scratch-wound healing assay revealed a significant acceleration in wound closure at 24 h by 58.09% (GF5) and 57.45% (GC2). The potential for free thymol hydrogel, GF5, and GC2 to combat MRSA in a murine skin model was evaluated. The bacterial counts, recovered from skin lesions and the spleen, were assessed. Although a significant reduction in the bacterial counts recovered from the skin lesions was shown by all three formulations, only GF5 and GC2 were able to reduce the bacterial dissemination to the spleen. Thus, our study suggests that Eudragit RS30D nanoparticles-based hydrogels are a potential delivery system for enhancing thymol skin retention and wound healing activity.

Formulation and Characterization of Mucoadhesive Microspheres of Oxazolidines Class Drug for the Treatment of Loosen Enteritis

This study aimed to developed novel fast disintegrating sustained release pellets containing tablet by using Fluidized Bed processor. Verapamil HCl used as a model drug for the formulation. Fluidized bed processor was used for coating of drug and polymer on the sugar spheres. To overcome the problem of swallowing for paediatric, geriatric, psychiatric, bedridden patients, uncooperative patients or for active patients who are busy and travelling and may not access to we aim to formulate the fast-disintegrating tablet. The superdisintigrant are commonly use like cross povidone, sodium starch glycolate which disintegrate tablet rapidly. It is assumed that, after the disintegration of tablets, pellets within tablets which are reside in GIT for several hours and gradually released a drug in controlled way. Eudragit RS 30D and ethyl cellulose were used as a sustained release polymer. Coating of spheres with sustained release film is achieved by bottom spray processor of FBP. Proper pellets coating film thickness, and concentration of polymers’, ensure obtaining desirable VH release profile for extended period of time, was defined. X composition of tablet with pellets were examined in order to obtained formulation, from which VH release would mostly appropriate pellets before compressing. Compression of pellets into tablet, being a modern technological process than enclosing them into hard gelatine capsule. The optimized batch evaluated by studied the effect of compression force, tablet hardness and friability and drug release from the pellets by sustained release manner.

Formulation and Evaluation of Captopril Sustained Release Pellet Containing Tablet by Fluidized Bed Processing

A novel compression of coated pellets formulation of captopril was developed in order to improve the efficacy of antihypertensive therapy considering the half-life of drug. The sustained release pellets containing tablet were prepared by using 32 factorial design by employing 2 polymers i.e., HPMC k4M and eudragit RS 30D at 3 levels. As captopril having short half-life (2 hrs) there is need to formulate the modified release formulation. sustained release pellets containing tablet is the best approach to reduce the dose frequency of captopril tablet, by using the single polymer (eudragit RS 30D). The release retardant layer over a drug loaded pellets was achieved by 3% eudragit RS 30D polymer solution by using fluidized bed processor and then the pellets were mixed with other excipients and compress into the tablets and it showed the good sustained release pattern.

Formulation Development and Evaluation of Fast Disintegrating Sustained Release Pellets Containing Verapamil Hydrochloride Tablets by Fluidized Bed Processor

This study aimed to developed novel fast disintegrating sustained release pellets containing tablet by using Fluidized Bed processor. Verapamil HCl used as a model drug for the formulation. Fluidized bed processor was used for coating of drug and polymer on the sugar spheres. To overcome the problem of swallowing for paediatric, geriatric, psychiatric, bedridden patients, uncooperative patients or for active patients who are busy and travelling and may not access to we aim to formulate the fast-disintegrating tablet. The superdisintigrant are commonly use like cross povidone, sodium starch glycolate which disintegrate tablet rapidly. It is assumed that, after the disintegration of tablets, pellets within tablets which are reside in GIT for several hours and gradually released a drug in controlled way. Eudragit RS 30D and ethyl cellulose were used as a sustained release polymer. Coating of spheres with sustained release film is achieved by bottom spray processor of FBP. Proper pellets coating film thickness, and concentration of polymers’, ensure obtaining desirable VH release profile for extended period of time, was defined. X composition of tablet with pellets were examined in order to obtained formulation, from which VH release would mostly appropriate pellets before compressing. Compression of pellets into tablet, being a modern technological process than enclosing them into hard gelatine capsule. The optimized batch evaluated by studied the effect of compression force, tablet hardness and friability and drug release from the pellets by sustained release manner.

Development and In Vitro Evaluation of a Novel Pulsatile Drug Delivery System Containing Dexketoprofen Trometamol

A pulsatile drug delivery system containing dexketoprofen trometamol was designed by combining immediate release and colon-targeted mini tablets into a capsule. Both immediate release and colon-targeted mini tablets were prepared by wet granulation. Furthermore, colon-targeted mini tablets were coated with Eudragit L 100, Eudragit S 100, Eudragit RS 30D, and ethylcellulose (Surelease®) using Wurster and pan coating methods. The optimum drug release of the system developed in the study was found to be mini tablets coated with 30% Eudragit S 100 on a 20% Surelease® subcoating for the purpose of colon targeting. In the finished product, the immediate release part released the drug within the first hour, and less than 5% release was observed from the colon-targeted tablets in a 0.1 N HCl in 2 h. Then, less than 20% release occurred in the colon-targeted tablets up to 6 h in pH 6.8 phosphate buffer solution. The cumulative release rate reached 100% for up to 12 h. To our knowledge, it was the first time dexketoprofen trometamol was designed by combining both immediate release and colon-targeted mini tablets in a one dosage form.

Application of Eudragit RS 30D as a Potential Drug Release Retardant of Acetaminophen and Caffeine for Prolonged Duration of Comfort

The objective of the study is to formulate an extended release matrix tablet dosage form containing acetaminophen and caffeine by applying polymer technology which will relieve all kinds of pain for about 12 hours. Considering the fact that there is no such formulation available in the pharmaceutical market, it is expected that this drug could be an effective introduction. Hydrophobic polymers have a great application in pharmaceutical sciences as they retard the release of water-soluble drugs and give prolonged effect. Eudragit RS 30D was used to prepare 3 formulations (EF1, EF2, and EF3) containing varying concentrations of polymer, through the wet granulation method. Each tablet contained 1000 mg of acetaminophen and 130 mg of caffeine including other suitable excipients. All pharmacopeial and nonpharmacopeial tests were conducted to determine the quality of dosage form and to identify optimized formulation among EF1-EF3. Dissolution was conducted on similar gastric conditions through which different kinetic models were applied using DDSolver. For 12 hrs of dissolution, caffeine was released from EF1, EF2, and EF3 with the percentage release in the range from 99.85% to 100.65%, 99.32% to 100.28%, and 98.09% to 100.77%, respectively. For acetaminophen, the percent release was from 99.81% to 100.91%, 100.24% to 100.91%, and 86.81% to 95.73% for EF1-EF3, respectively. Results concluded that EF2 is the most optimized drug having all physicochemical quality control tests within the specified limits. On applying different models like zero-order, Hixson-Crowell, Higuchi, and Korsmeyer-Peppas upon use, it is concluded that the formulation follows Korsmeyer-Peppas as it was the best-fitted model with the r2 value closest to 0.999. EF2 is considered as a potential drug to be manufactured that will give prolonged relief against pain and will decrease compliance issues related to dosing frequency.

Optimizing pH-sensitive and time-dependent polymer formula of colonic pH-responsive pellets to achieve precise drug release

Time-sensitive and pH-dependent polymers are generally employed to prepare colon-site delivery system, and their coating thickness and order are very important in controlling the drug release. The traditional colon-site delivery systems consist of time-dependent polymers as inner layer and pH-sensitive polymers as outer layer. However, they suffer from low drug-loading rate and immature drug release. In this study, total alkaloids of sophora alopecuroides(TASA)-loaded pellets were prepared by extrusion-spheronization method and coated with Eudragit RS30D and Eudragit S100. Pellets using Eudragit RS30D as inner layer and Eudragit S100 as outer layer were named as ERS-ES100 TCO, while pellets with Eudragit S100 as inner layer and Eudragit RS30D as outer layer were ES100-ERS NCO. Both types of formulations with varying coating ratios and orders of Eudragit S100 and Eudragit RS30D were designed and prepared. The following in vitro drug release and SEM studies indicated that ERS-ES100 TCO(F2) with 12.8% Eudragit RS30D as inner layer and 21% Eudragit S100 as outer layer released up to 42% drug in 5 h. Interestingly, ES100-ERS NCO (F4) coated with 12.8% Eudragit S100 and 14.8% Eudragit RS30D showed optimal drug release in colon. In conclusion, ES100-ERS NCO colonic delivery system achieved reduced coating thickness and improved colonic targeting compared with traditional delivery system (ERS-ES100 TCO). In addition, the similarity factors (f2) value of sophoridine and matrine for investigated formulation were within 50–100 and > 80, demonstrating that sophoridine and matrine in all formulations achieved a synchronous release.

Preparation of Colon-specific and Synchronous Release Pellet Containing Total Alkaloids of Sophora alopecuroides

ObjectiveTo deliver multiple component drugs to colon site and sustain a synchronous release for better therapeutic effect. For achieving this purpose, colon specific pellet containing total alkaloids of Sophora alopecuroides (TASA) was prepared. MethodsThe pellet was prepared by extrasion-spheronizing and subsequently coated with three layers of two polymers. ResultsThe pellet core consisted of 40% TASA, 1:2 in ratio of Bletilla striata polysaccharide (BSP), an enzyme-degradable material, to microcrystalline cellulose (MCC), filler, and 1% CMC-Na solution as binder by optimization. Concerning of the three coated layers, the outer layer was coated with Eudragit RS30D for controlling drug release in colon, the intermediate layer and the inner layer were coated with same polymer, Eudragit S100, for preventing drug release in upper gastrointestinal tract, which required 23.2%, 21.7%, and 9.3% weigh gain, respectively. The coated pellets released 1.20% of sophoridine and 1.98% of matrine in media mimicking the stomach condition for 2 h, and 23.88% of sophoridine and 22.91% of matrine in media mimicking the intestine for 3 h and finally 90.25% of sophoridine and 89.94% of matrine in colonic conditions within 24 h. And the similarity factor f of sophoridine and matrine of release curve for investigated formulation was internal in (50–100) and > 80, demonstrating that sophoridine and matrine in formulation achieved a synchronous release. ConclusionThe coated pellets achieve a certain colon-specific release and synchronous release.

Evaluation of blank film forming polymeric dispersions based on Eudragit RL 30D and RS 30D for transdermal drug delivery

Evaluation of blank film forming polymeric dispersions based on Eudragit RL 30D and RS 30D for transdermal drug delivery

Surface Deposition and Coalescence and Coacervation Phase Separation Methods: In Vitro Study and Compatibility Analysis of Eudragit RS30D, Eudragit RL30D, and Carbopol-PLA Loaded Metronidazole Microspheres.

Metronidazole (MTZ) has extremely broad spectrum of protozoal and antimicrobial activity and is clinically effective in trichomoniasis, amoebic colitis, and giardiasis. This study was performed to formulate and evaluate the MTZ loaded microspheres by coacervation phase separation and surface deposition and coalescence methods using different polymers like Gelatin, Carbopol 934P, Polylactic Acid (PLA), Eudragit RS30D, and Eudragit RL30D to acquire sustained release of drug. In vitro dissolution studies were carried out in phosphate buffer (pH 7.4) for 8 hours according to USP paddle method. The maximum and minimum release of MTZ from microspheres observed were 84.81% and 76.6% for coacervation and 95.07% and 80.07% for surface deposition method, respectively, after 8 hours. Release kinetics was studied in different mathematical release models. The SEM and FTIR studies confirm good spheres and smooth surface as well as interaction between drug and polymers. Though release kinetic is uncertain, the best fit was obtained with the Korsmeyer kinetic model with release exponent (n) lying between 0.45 and 0.89. In vitro studies showed that MTZ microspheres with different polymers might be a good candidate as sustained drug delivery system to treat bacterial infections.

Effect of Antiadherents on the Physical and Drug Release Properties of Acrylic Polymeric Films

Antiadherents are used to decrease tackiness of a polymer coating during both processing and subsequent storage. Despite being a common excipient in coating formulae, antiadherents may affect mechanical properties of the coating film as well as drug release from film-coated tablets, but how could addition of antiadherents affect these properties and to what extent and is there a relation between the physical characteristics of the tablet coat and the drug release mechanisms? The aim of this study was to evaluate physical characteristics of films containing different amounts of the antiadherents talc, glyceryl monostearate, and PlasACRYL(TM) T20. Eudragit RL30D and Eudragit RS30D as sustained release polymers and Eudragit FS30D as a delayed release material were used. Polymer films were characterized by tensile testing, differential scanning calorimetry (DSC), microscopic examination, and water content as calculated from loss on drying. The effect of antiadherents on in vitro drug release for the model acetylsalicylic acid tablets coated with Eudragit FS30D was also determined. Increasing talc concentration was found to decrease the ability of the polymer films to resist mechanical stress. In contrast, glyceryl monostearate (GMS) and PlasACRYL produced more elastic films. Talc at concentrations higher than 25% caused negative effects, which make 25% concentration recommended to be used with acrylic polymers. All antiadherents delayed the drug release at all coating levels; hence, different tailoring of drug release may be achieved by adjusting antiadherent concentration with coating level.

Formulation and in vitro characterization of poly(dl-lactide-co-glycolide)/Eudragit RLPO or RS30D nanoparticles as an oral carrier of levofloxacin hemihydrate

The main objective of this study was to design positively charged Levofloxacin Hemihydrate (Levo-h)-loaded nanoparticles with improved entrapment efficiency and antibacterial activity. PLGA alone or in combinations with Eudragit® RLPO or RS30D with or without positively charged inducing agent; 1,2-dioleoyl-3-trimethylammonium-propane, chloride salt (DOTAP); were used for preparation of nanoparticles. Blending between PLGA and Eudragit® RLPO or RS30D with inclusion of DOTAP caused a marked increase in entrapment efficiency and switched zeta potential from negative to positive. Nanoparticle formulations; NR3 (Levo-h:PLGA:Eudragit® RLPO; 1:1:1 w/w with DOTAP) and NS3 (Levo-h:PLGA:Eudragit® RS30D; 1:1:1 w/w with DOTAP) that possess high positive zeta potential (59.3 ± 7.5 and 55.1 ± 8.2 mV, respectively) and Efficient Levo-h entrapment (89.54 ± 1.5 and 77.65 ± 1.8%, respectively) were selected for further examinations; in vitro release, physical stability and microbiological study. NR3 and NS3 showed significant sustained release of Levo-h. NR3 and NS3 exhibited good stability after storage at room temperature. Microbiological assay showed strengthened antibacterial activity of NR3 against both types of gram-negative bacteria (E. coli, Ps. aeruginosa) and of NS3 against Ps. aeruginosa compared to free Levo-h solution. NR3 and NS3 appear to be promising oral delivery system for Levo-h.

Design and Evaluation of a Novel Gas Formation-Based Multiple-Unit Gastro-Retentive Floating Drug Delivery System for Quetiapine Fumarate

Purpose: To develop a gastro-retentive formulation of quetiapine fumarate in the form of floating minitablets.Methods: The system consisted of core units prepared by direct compression process, which were coated with three successive layers, namely, an inner seal coat, effervescent layer and an outer polymeric layer of polymethacrylates.Results: Mini-tablets coated with Eudragit RS 30D (5, 7.5 and 10%) released . 85% of the drug after 12 h, while those coated with Eudragit RL 30D (5, 7.5 and 10%) released . 85% drug within the same period. Drug release kinetic studies showed that drug diffusion fitted best to zero order and Higuchi models, indicating that drug release was anomalous non-Fickian transport. In vivo gastric residence time results indicate that the units remained in the stomach for about 6 h (n = 3). There was nosignificant change in dissolution profiles before and after storage at 40‹C and 75% RH for 6 months.Conclusion: The developed floating mini-tablets of quetiapine fumarate exhibit prolonged release for .12 h, and thus may improve bioavailability and minimize fluctuations in plasma drug concentrations. Keywords: Mini-tablets; Floating delivery system; Effervescence, Polymeric membrane, Controlled release, Quetiapine fumarate

Quaternary polymethacrylate–magnesium aluminum silicate films: Molecular interactions, mechanical properties and tackiness

The aim of this study was to investigate the impact of the addition of magnesium aluminum silicate (MAS), a natural clay, on the properties of polymeric films based on quaternary polymethacrylates (QPMs). Two commercially available aqueous QPM dispersions were studied: Eudragit(®) RS 30D and Eudragit(®) RL 30D (the dry copolymers containing 5 and 10% quaternary ammonium groups, respectively). The composite QPM-MAS films were prepared by casting. Importantly, QPM interacted with MAS and formed small flocculates prior to film formation. Continuous films were obtained up to MAS contents of 19% (referred to the QPM dry mass). ATR-FTIR and PXRD revealed that the positively charged quaternary ammonium groups of QPM interacted with negatively charged SiO(-) groups of MAS, creating nanocomposite materials. This interaction led to improved thermal stability of the composite films. The puncture strength and elongation at break of dry systems decreased with increasing MAS content. In contrast, the puncture strength of the wet QPM-MAS films (upon exposure to acidic or neutral media) increased with increasing MAS content. Furthermore, incorporation of MAS into QPM films significantly decreased the latter's tackiness in the dry and wet state. These findings suggest that nanocomposite formation between QPM and MAS in the systems can enhance the strength of wet films and decrease their tackiness. Thus, MAS offers an interesting potential as novel anti-tacking agent for QPM coatings.

Capsaicin Injectable <i>In-Situ</i> Forming Gels

Capsaicin exhibits the analgesic and anti-inflammatory activities, therefore it is interesting to apply this natural active compound for periodontitis treatment by local drug delivery system such as intra-canal route. Capsaicin in-situ forming gels were prepared in this research work. The viscosity, gel forming property and capsaicin release were evaluated. 30%W/W eudragit RS 30D in N-methylpyrrolidone (NMP) employed as gel base was physicaly stable after sterilization with autoclaving and exhibited the in-situ forming gel property. This gel base was still clear when capsaicin was less than 0.0094 %w/w. When the system contacted with phosphate buffer pH 6.8 the turbid gel was appeared rapidly at the interface. Viscosity of system depended on the amount of eudragit RS 30D. The rheology of systems was newtonian flow and amount of capsaicin tincture did not affect the rheological behavior. The release rate and amount of capsaicin release form gels were lower than those of capsaicin solution. The sustainable release of capsaicin could be obtained from the developed in-situ forming gel.

Preparation and Evaluation of a Gas Formation-based Multiple-Unit Gastro-Retentive Floating Delivery System of Dipyridamole

The aim of this study was to prepare mini tablets to be filled into a capsule that is designed to float on the gastric contents based on gas formation technique. The drug-containing core mini-tablets were prepared by wet granulation method followed by a coating of the core units with seal coating, an effervescent layer and a gas-entrapping polymeric membrane (Eudragit RS30D, RL30D). Dipyridamole, which is predominantly absorbed in the upper part of GI tract and unabsorbed/insoluble at the lower intestine, was used as a model drug. The effect of the preparative parameters like amount of the effervescent agent layered onto the seal coated units, type and coating level of the gas-entrapping polymeric membrane, floating ability and drug release properties of the multiple-unit FDDS were evaluated. The formulations were evaluated for pharmacopoeial quality control tests. Physical parameters were found to be within the acceptable limits. The system using Eudragit® RL30D as a gas-entrapping polymeric membrane exhibited floating properties. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapping polymeric membrane decreased. The optimum system exhibited complete floating within 3 minutes and maintained that buoyancy over a period of 8 hours. The drug release was sustained and linear with the square root of time. Increasing the coating level of the gas-entrapping polymeric membrane decreased drug release. Both the rapid-floating and sustained-release properties were achieved in the multiple-unit floating delivery system developed in this study. The in vivo gastric residence time was examined by radiograms and it was found that the units remained in the stomach for about 6 hours. The analysis of the dissolution data after storage at 40°C and 75% RH for 6 months showed no significant change indicating good stability.

Preparation and in vitro/in vivo evaluation of a ketoprofen orally disintegrating/sustained release tablet

Context: Orally disintegrating tablets (ODTs) with sustained release profiles are a new generation of ODTs called orally disintegrating/sustained release tablets (ODSRTs), which are convenient in use and able to slowly release drugs to maintain effective blood concentrations over a prolonged period of time. Ketoprofen, one of non-steroidal anti-inflammatory drugs, is an ideal model drug for ODSRTs.Methods: We designed a simple two-step process to develop novel ketoprofen orally disintegrating/sustained release tablets (KODSRTs). Firstly, sustained release ketoprofen fine granules were developed by spray drying the aqueous dispersions composed of Eudragit RS-30D, Starch 1500 and PEG 6000. The optimal parameters of spray drying were 100°C for inlet air temperature and 1.5 mL/min for feed rate. Subsequently, the obtained granules were directly compressed into KODSRTs after mixing with lactose, mannitol and a superdisintegrant, crosslinked polyvinylpyrrolidone (PVPP). The characteristics of KODSRTs, especially their potential for extended drug release, were evaluated.Results: Results of an in vitro release test demonstrated that KODSRTs could slowly release ketoprofen for 24 h after disintegrating within 30 s. Extended release properties of KODSRTs were decided by the ketoprofen sustained release fine granules in tablets. Besides, the disintegration time of KODSRTs depended on the percentage of PVPP in tablets. In vivo pharmacokinetic studies in beagles also showed that KODSRTs possessed a significantly extended release profile compared with ketoprofen normal capsules.Conclusion: KODSRTs were successfully prepared using a simple two-step process: spray drying and direct compression.

DEVELOPMENT OF SUSTAINED RELEASE TABLET OF METFORMIN HYDROCHLORIDE BY AQUEOUS COATING

The aim of present work was to develop a metformin hydrochloride sustained release tablet by aqueous coating. Eudragit RL and Eudragit RS were used for coating of tablets. Eudragit RL having 10% and Eudragit RS having 5% of functional quaternary ammonium groups, which give rise to pH independent permeability of the polymer. Metformin hydrochloride uncoated tablets were prepared by wet granulation technique. Tablets were coated with blends of Eudragit RS30D and Eudragit RL30D in 5:1 and in 3:1 ratios at different coating level viz. 7%, 5%, 3%, 1.5%, 1%. Two dissolution media: pH 1.2 and pH 6.8 phosphate buffer were employed for in vitro release behaviors of metformin hydrochloride tablets. Coating with blends of Eudragit RS 30D and Eudragit RL 30D in 5:1 and in 3:1 ratio at 1% and at 3% showed sustained release effect for 12 h. The two Eudragit polymers with different features as coating materials produced the desired results.

Pectin Film Coated Pellets for Colon-targeted Delivery of Budesonide: In-vitro/In-vivo Evaluation in Induced Ulcerative Colitis in Rat.

The main objective of this study was to prepare colon-specific pellets of budesonide, using pectin as film coating. Pellet cores of budesonide were prepared by extrusion / spheronization technique. Pectin, in different ratios was combined with Eudragit RS30D, Eudragit NE30D or Surelease to produce film coating. The dissolution profiles of pectin coated pellets were investigated in pH of 1.2 (2 h), pH of 7.4 (4 h) and pH of 6.8 in the absence as well as presence of rat cecal contents (18 h). Finally the selected formulation was evaluated on trinitrobenzenesulfonic acid (TNBS) induced ulcerative colitis in rat model, in comparison with conventional UC treatments. The dissolution profiles of pectin coated pellets showed that the release of budesonide in presence of rat cecal content depended on adjuvant polymer, the ratio of pectin to polymer and film thickness. Coated pellets, prepared out of pectin and Surelease at a ratio of 1:3 at coating level of 35% (w/w), could increase budesonide release statistically in presence of rat cecal content, while they released no drug in pH of 1.2 and 7.4. Animal experiments revealed the therapeutic efficacy of pectin/Surelease-coated pellets of budesonide in alleviating the conditions of TNBS-induced colitis model as reflected by weight gain, as well as improvement of clinical, macroscopic and microscopic parameters of induced colitis. This confirmed the ability of the optimized formulation for targeted drug delivery of budesonide to colon.

Design, Evaluation and Statistical Optimization of Diazepam Loaded Controlled Release Micropellets

This work aims at designing and evaluating a Extended release dosage form of Diazepam using Alginate- Eudragit RS 30D as the matrix-forming polymer employing the Ionotropic Gelation technique of micropellletization. The product was characterized by physicochemical parameters such as yield, drug entrapment efficiency, particle size, surface topography, granulometric study, loose surface crystal study, drug-excipient compatibility and in vitro release. The controlled release profile was optimized using a factorial design for achieving the correct blend of microparticles that closely matches the target release profile. The study illustrates the utility and advantage of designed experimentation in controlled drug delivery research.