Formulation and characterization of ethylcellulose microparticles containing .l-alanyl- l-glutamine peptide

Context: The l-alanyl-l-glutamine peptide (AGP) has been effective to promote acute glycemia recovery during long-term insulin-induced hypoglycemia (IIH), and the oral administration of AGP is suggested to prevent prolonged hypoglycemia, such as nocturnal hypoglycemia.

Objective: Considering the ability of AGP on glycemia recovery and AGP’s fast metabolism, the aim of current study was to obtain and characterize ethylcellulose microparticles to deliver the drug for a prolonged time.

Materials and Methods: Microparticles were prepared by simple and double emulsification/hardening method and characterized by scanning electron microscopy, thermogravimetry (TG), differential scanning calorimetry (DSC), Fourier transform infra-red (FTIR) and FT-Raman spectroscopy and in vitro release.

Results and Discussion: Spherical structures with a mean diameter between 9.30?µm and 13.19?µm were formed. TG analysis showed that the thermal stability of AGP was even more increased by encapsulation with ethylcellulose. In addition, TG, DSC, FTIR and FT-Raman analyses proved that AGP was encapsulated in a molecular way. Higher values of encapsulation efficiency were observed for the microparticles prepared by double emulsification (57.83–83.67%) than for those prepared by simple emulsification (18.37%). However, the last ones could release the peptide in a quicker and more extensive manner than those prepared by double emulsification.

Conclusion: For the first time, microparticles containing AGP were developed and exhibited prolonged in vitro release as well as protection to the drug, and it could be considered as a dosage form for patients who suffer from insulin-induced hypoglycemia and/or nocturnal hypoglycemia.     

Nifedipine Molecular Dispersion in Microparticles of Ammonio Methacrylate Copolymer and Ethylcellulose Binary Blends for Controlled Drug Delivery: Effect of Matrix Composition

ABSTRACT

The objective of this study is to explore matrix-type microparticles, comprising a solid dispersion of drug with an ammonio methacrylate copolymer and ethylcellulose binary blend, for use in the controlled release of a poorly water-soluble drug, nifedipine. Microparticles consisting of an ethylcellulose N7 (N7) and Eudragit RL® (RL) binary blend at different ratios were prepared using phase-separation methodology. The effects of matrix composition on microparticle properties were evaluated by polarized light microscopy, differential scanning calorimetry (DSC), FT-infrared and UV-visible spectroscopy, stability, and drug release studies. Study results indicate that the particle size distribution, particle morphology, and drug release rate from the microparticles were influenced by the ratio of RL to N7. Discrete spherical microparticles with a narrow size distribution and a controlled release profile were obtained when the ratio of RL to N7 was in the range from 1:1 to 2:1 w/w. Solid-state characterization and release kinetic studies on these microparticles confirmed that the nifedipine release from the microparticles followed the Baker and Lonsdale's matrix diffusion model (1974) for microspheres containing dissolved drug, and the nifedipine diffusion in the microparticle matrix was the rate-limiting step. As the ratio of RL to N7 was changed from 0:1 to 4:1 w/w, the effective drug diffusion coefficient in the micro-matrix increased from 5.8?×?10^?10 to 8.6?×?10^?9 (cm²/h). In addition, probably due to formation of a stable molecular dispersion promoted by hydrogen bonding between nifedipine and the polymers, no significant changes in the nifedipine physical form or release kinetics were observed after 1-year storage at ambient room temperature followed by 3-month accelerated stability at 40°C/75% RH in a closed container.     

Nifedipine molecular dispersion in microparticles of ammonio methacrylate copolymer and ethylcellulose binary blends for controlled drug delivery: effect of matrix composition

The objective of this study is to explore matrix-type microparticles, comprising a solid dispersion of drug with an ammonio methacrylate copolymer and ethylcellulose binary blend, for use in the controlled release of a poorly water-soluble drug, nifedipine. Microparticles consisting of an ethylcellulose N7 (N7) and Eudragit RL® (RL) binary blend at different ratios were prepared using phase-separation methodology. The effects of matrix composition on microparticle properties were evaluated by polarized light microscopy, differential scanning calorimetry (DSC), FT-infrared and UV-visible spectroscopy, stability, and drug release studies. Study results indicate that the particle size distribution, particle morphology, and drug release rate from the microparticles were influenced by the ratio of RL to N7. Discrete spherical microparticles with a narrow size distribution and a controlled release profile were obtained when the ratio of RL to N7 was in the range from 1:1 to 2:1 w/w. Solid-state characterization and release kinetic studies on these microparticles confirmed that the nifedipine release from the microparticles followed the Baker and Lonsdale's matrix diffusion model (1974) for microspheres containing dissolved drug, and the nifedipine diffusion in the microparticle matrix was the rate-limiting step. As the ratio of RL to N7 was changed from 0:1 to 4:1 w/w, the effective drug diffusion coefficient in the micro-matrix increased from 5.8 × 10^-10 to 8.6 × 10^-9 (cm²/h). In addition, probably due to formation of a stable molecular dispersion promoted by hydrogen bonding between nifedipine and the polymers, no significant changes in the nifedipine physical form or release kinetics were observed after 1-year storage at ambient room temperature followed by 3-month accelerated stability at 40°C/75% RH in a closed container.     

Preparation and Characterization of Heparin-Loaded Polymeric Microparticles

ABSTRACT

Microparticles containing heparin were prepared by a water-in-oil-in-water emulsification and evaporation process with pure or blends of biodegradable (poly-?-caprolactone and poly(d,l-lactic-co-glycolic acid)) and of positively-charged non-biodegradable (Eudragit® RS and RL) polymers. The influence of polymers and some excipients (gelatin A and B, NaCl) on the particle size, the morphology, the heparin encapsulation rate as well as the in vitro drug release was investigated. The diameter of the microparticles prepared with the various polymers ranged from 80 to 130 µm and was found to increase significantly with the addition of gelatin A into the internal aqueous phase. Microparticles prepared with Eudragit RS and RL exhibited higher drug entrapment efficiency (49 and 80% respectively), but lower drug release within 24 h (17 and 3.5% respectively) than those prepared with PCL and PLAGA. The use of blends of two polymers in the organic phase was found to modify the drug entrapment as well as the heparin release kinetics compared with microparticles prepared with a single polymer. In addition, microparticles prepared with gelatin A showed higher entrapment efficiency, but a significant initial burst effect was observed during the heparin release. The in vitro biological activity of heparin released from the formulations affording a suitable drug release has been tested by measuring the anti-Xa activity by a colorimetric assay with a chromogenic substrate. The results confirmed that heparin remained unaltered after the entrapment process.     

Preparation and in vivo evaluation of spray dried matrix type controlled-release microparticles of tamsulosin hydrochloride for orally disintegrating tablet

The objective of this study was to achieve an optimal formulation of spray dried matrix type controlled-release (MTCR) microparticles containing tamsulosin hydrochloride for orally disintegrating tablet. To control the release rate of tamsulosin hydrochloride, Acrylate-methacrylate copolymer (Eudragit^® L-100 or Eudragit^® S-100) and ethylcellulose were employed on the composition of MTCR microparticles. Physicochemical properties of MTCR microparticles such as particle size and SEM were characterized. Pharmacokinetic parameters of tamsulosin hydrochloride were evaluated in the rats after oral administration. MTCR microparticles were spherical microparticles of around 10 µm diameter with a corrugated surface. ODTs containing MTCR microparticles were disintegrated within 30 s and MTCR microparticles were able to control the release rate of tamsulosin hydrochloride following Fickian diffusion mechanism. The in vitro release rates of tamsulosin hydrochloride from MTCR microparticles were proportional to the ratio of Acrylate-methacrylate copolymer to ethylcellulose. Moreover, MTCR microparticles retarded the in vivo release rate of tamsulosin hydrochloride without reducing the bioavailability. Our results suggest that MTCR microparticles may be potential oral dosage forms to control the release and to improve the bioavailability of tamsulosin hydrochloride.     

Controlled-Release Matrix of Acetaminophen-Ethylcellulose Solid Dispersion

Abstract

In this study ethylcellulose was evaluated as a carrier for preparation of prolonged release acetaminophen tablets. Solid dispersions containing three levels of ethylcellulose and acetaminophen (1:3; 1:1; 3:1) were prepared by the solvent method. Also physical mixtures at the same level of ethylcellulose and acetaminophen were prepared. Systems composed of solid dispersion or physical mixture containing the equivalent weight of 50 mg acetaminophen, Lactose fast-flo as diluent and 1% magnesium stearate as lubricant were compressed into tablets and tested for dissolution. The dissolution data showed that the drug release decreased as the level of ethylcellulose increased in the solid dispersion formulations. The drug release from tablets prepared with solid dispersion followed the diffusion controlled model for inert porous matrix, while the drug release from tablets prepared with physical mixture followed the first-order kinetic model.     

Evaluation of Ethylcellulose as a Matrix for Prolonged Release Formulations. II. Sparingly Water-Soluble Drugs: Ibuprofen and Indomethacin

Abstract

The main purpose of this investigation was to evaluate ethylcellulose as a carrier for the preparation of prolonged release solid dispersions of sparingly water-soluble drugs, ibuprofen and indomethacin. Solid dispersions containing various concentrations of ethylcellulose of different viscosity grades were prepared by the solvent method. Tablets were directly compressed from solid dispersions (40/100 mesh) with 0.5% Primojel as a disintegrant and 0.5% magnesium stearate as a lubricant. In vitro release studies employed a rotating bottle system with Sorenson's buffer solution (pH 7.4). It was found that prolongation of drug release was primarily associated with an increase in amount of ethylcellulose rather than the viscosity grade. Nonetheless, the higher the viscosity grade of ethylcellulose, the slower the release of drug from granular and compressed solid dispersions. The release rate of ibuprofen was faster than that of indomethacin from different solid dispersion formulations.     

Controlled release antibiotics for dry powder lung delivery

Introduction: Two controlled release (CR) antibiotics intended for inhalation therapy were evaluated. Material and Methods: Ciprofloxacin and doxycycline (both hydrochlorides) were selected as model drugs. Microparticles containing 90:10 ratio of polyvinyl alcohol (PVA) and single antibiotics or combinations were obtained via spray drying. The microparticles were evaluated in terms of particle size, morphology, thermal properties, aerosol performance, and in vitro release. Results and Discussion: Analysis of the microparticle morphology indicated comparable size distributions (2.04 ± 0.06, 2.15 ± 0.01, and 2.21 ± 0.01 μm for ciprofloxacin, doxycycline, and co-spray-dried antibiotic formulations, respectively). Thermal analysis of the microparticles suggested similar responses, which were dominated by the endothermic peaks observed for PVA alone. Analysis of the aerosol performance suggested that the individual antibiotic formulations had different aerosol profiles that were dependent on the antibiotic used. In comparison, the combination CR antibiotics had identical aerosol profiles, suggesting that the microparticles were homogeneous. The release of antibiotics from the CR microparticles showed that ≤50% was released over a 6-hour period in comparison to ≥90% being released in the first hour for microparticles containing no PVA. Conclusions: The potential for antibiotic therapy, and specifically CR antibiotic therapy using dry powder inhalers, provides a promising route for the treatment of pulmonary infection.     

Preparation And Evaluation of A Long Acting Liquied Antitussive Product

Abstract

Microparticles containing a dextramothophan-resins complex were prepared by a modified emulsion solvent evaporation method. The particles were evaluated for size distribution and dissolution rate. Selected microparticles were suspended in various liquid media and stored at room tempertature. Dissolution of suspended in various liquid media and stored at room temperature. Dissolution of suspended microparticles was studied after storage up to 40 days. The particles were found to be stable and did not release drug in a supending media containing 30% propylene glycol, 35% syrup and 35% of 1% methylcellulose 1500 cps solution.     

Microparticles of poly(hydroxybutyrate-co-hydroxyvalerate) loaded with andiroba oil: Preparation and characterization

Poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV), a biodegradable polyester, was used in the preparation of polymeric microparticles containing andiroba oil. Andiroba oil, extracted from the seeds of Carapa guianensis, has insecticide and medicinal properties. Microparticles of PHBV were prepared using o/w simple emulsion followed by solvent evaporation. The properties of these microparticles, such as encapsulation efficiency, and morphological aspects were investigated. Several characterization techniques were used: FTIR, XRD, DSC, TGA-DTA, SEM, and particle-size analysis. The efficiency of encapsulation of andiroba oil was determined by UV-spectroscopy. The results confirmed that PHBV microspheres containing andiroba oil were obtained.     

Comparison of simple Eudragit microparticles loaded with prednisolone and Eudragit-coated chitosan-succinyl-prednisolone conjugate microparticles: Part I. Particle characteristics and in vitro evaluation as a colonic delivery system

Objective: Simple Eudragit microparticles loaded with prednisolone and chitosan-succinyl-prednisolone conjugate microparticles coated with Eudragit were prepared and characterized in vitro in order to obtain their basic features as a colonic delivery system.

Materials and methods: Both types of microparticles were prepared by the emulsification-solvent evaporation modified somewhat from the previous one. Their particle size, shape and their drug content were investigated, and in vitro release profiles were examined using JP-15 1st fluid (pH 1.2), JP-15 2nd fluid (pH 6.8) and PBS (pH 7.4) as release media. Furthermore, the regeneration of conjugate microparticles from Eudragit-coated microparticles was investigated under the same incubation conditions.

Results: Simple Eudragit S100 (EuS) microparticles (ES-M) were almost spherical, ca. 1.2 μm diameter, and PD content ca. 3.7% (w/w). Conjugate microparticles (CS-M1) and EuS-coated conjugate microparticles (CS-M1/S) had particle sizes of ca. 2.8 and 15.3 μm, respectively, and PD contents of 5.4 and 2.1% (w/w), respectively. ES-M exhibited suppressed release at pH 1.2, gradual release at pH 6.8 and rapid release at pH 7.4. CS-M1 showed no release at pH 1.2, and very slow release at pH 6.8 and 7.4. CS-M1 regenerated poorly from CS-M1/S at pH 6.8.

Conclusions: Simple Eudragit micrparticles and Eudragit-caoted conjugate microparticles, prepared by the present methods, were found in vitro to be possibly useful as the delivery systems of PD to the lower intestine, although there were differences in their release rate and morphological features.     

Preparation and In Vitro Properties of N-Succinylchitosan– or Carboxymethylchitin–Mitomycin C Conjugate Microparticles with Specified Size

The preparation of cross-linked conjugate microparticles of N succinyl-chitosan (Suc) or 6-O-carboxymethylchitin (CM) with mitomycin C (MMC), which showed an adequate size for liver targeting (0.2–3 μm), was attempted by a combination of water-soluble carbodiimide (EDC) coupling and emulsification technique. As for Suc, microparticles with a diameter less than a few micrometers could be obtained easily, while the preparation of CM microparticles (CM-MPs) of the same diameter was not necessarily easy. First, preparation conditions were compared for CM-MPs, and some conditions gave CM-MPs with a diameter less than a few micrometers. As to CM-MMC conjugate microparticles, the method by addition of EDC after emulsification using CM with low molecular weight (CM_L) gave more appropriate microparticles with a mean diameter of 0.97 μm (CM_L-MP-MMC). Suc-MMC conjugate microparticles adequate for liver targeting could be produced by the addition of EDC both before and after emulsification; especially, the conjugate microparticles with a mean diameter of 0.45 μm (Suc-MP-MMC) were derived by the addition of EDC before emulsification. Suc-MP-MMC exhibited a higher drug content than CM_L-MP-MMC. CM_L-MP-MMC and Suc-MP-MMC exhibited 50% drug release times of 2.87 h and 42.1 h, respectively.     

Influence of lipid microparticle encapsulation on in vitro efficacy,photostability and water resistance of the sunscreen agents,octyl methoxycinnamate and butyl methoxydibenzoylmethane

Context: Essential requirements for the efficacy of sunscreen agents are optimal UV absorption, high photostability and resistance against water removal.

Objective: Aim of this study was to investigate the effect of encapsulation in lipid microparticles (LMs) on the overall performance of the two most commonly used sunscreen agents, octyl methoxycinnamate (OMC) and butyl methoxydibenzoylmethane (BMDBM).

Methods: LMs loaded with OMC and BMDBM were prepared by melt emulsification and characterized by optical microscopy, UV filter content and release studies. The LMs incorporating OMC and BMDBM or the nonencapsulated sunscreen agents were introduced into a model cream (oil-in-water emulsion).

Results: No significant differences were observed between the sun protection factor (SPF) of the formulations containing the free (SPF, 9.4?±?1.9) or microencapsulated (SPF, 9.6?±?1.3) UV filters. Irradiation of the creams with a solar simulator demonstrated that the photodecomposition of OMC and BMDBM was significantly decreased by encapsulation in LMs from 55.7?±?5.3% to 46.1?±?5.1% and 36.3?±?3.9% to 20.1?±?4.7%, respectively. However, in vitro water-resistance studies showed that entrapment in the LMs significantly enhanced the sunscreen agent removal caused by watering (the losses for OMC and BMDBM were 45.1?±?6.3% and 49.2?±?8.4%, respectively), as compared to the formulation with the nonencapsulated sunscreen agents (the losses for OMC and BMDBM were 26.7?±?6.1% and 28.0?±?6.7%, respectively).

Conclusion: Incorporation in LMs can have controversial effects on UV filter efficacy. In particular, the water-resistance properties of sun-care formulations containing sunscreens loaded in LMs should be verified to assure that the photoprotective activity is maintained during usage.     

Design and evaluation of acrylate polymeric carriers for fabrication of pH-sensitive microparticles

Colon-targeted microparticles loaded with a model anti-inflammatory drug were fabricated using especially designed acrylic acid–butyl methacrylate copolymers. Microparticles were prepared by oil-in-oil solvent evaporation method using Span 80 as emulsifier. Microparticles were found to be spherical in shape, hemocompatible and anionic with zeta potential of ?27.4 and ?29.0?mV. Entrapment of drug in the microparticles was confirmed by Fourier transform infrared (FTIR) spectroscopy. However, X-ray diffraction (XRD) and differential scanning calorimetry (DSC) revealed amorphous nature of microparticles due to the dilution effect of amorphous polymer. The microparticles released less than 5% drug at pH 1.2, while more than 90% of the drug load was released at pH 7.4. This suggested the colon targeting nature of the formulations. In experimentally developed colitis in Wistar rats, the microparticle formulation showed significant reduction (p?相似文献   

Influence of polymer blends on the characterization of gliclazide – encapsulated into poly (Æ-caprolactone) microparticles

Gliclazide (GLZ)-loaded microparticles made with a polymeric blend were prepared by a solvent evaporation technique. Organic solutions of two polymers, poly(?-caprolactone) (PCL) and Eudragit RS (E RS) or ethyl cellulose (EC), in different weight ratios, and 33.3% of GLZ were prepared and dropped into aqueous solution of poly vinyl alcohol, in different experimental conditions, achieving drug-loaded microparticles. The obtained microparticles were characterized in terms of yield of production, shape, size, surface properties, drug content, and in vitro drug release behavior. The physical state of the drugs and the polymer was determined by scanning electron microscopy (SEM), Fourier transform infra red and differential scanning calorimetry. Following the in vitro release studies microparticles made from blends of polymer, PCL/E RS or EC showed slower drug release than microparticles made from single PCL polymer. Surface morphology also revealed presence of porous and spherical structure of microparticles. Microparticles showing sustained release of GLZ were examined in rabbits and plasma GLZ concentrations were calculated using HPLC method of assay.     

Influence of polymers/excipients on development of agglomerated crystals of secnidazole by crystallo-co-agglomeration technique to improve processability

Background: Direct tabletting is a need of Pharmaceutical industries. Poor mechanical properties of drug particles require wet granulation which is uneconomical, laborious, and tedious.

Objective: Objective of this work was to study influence of various polymers/excipients on formation of directly compressible Crystallo-co-agglomerates (CCA) of water soluble drug Secnidazole (hydroxy-2-propyl)-1-methyl-2-nitro-5-imidazole), an antimicrobial agent.

Method: Acetone-petroleum ether system was used to develop CCA of drug in the presence of polymers/excipients. Clarity of the supernatant was considered an endpoint for completion of agglomeration. The prepared CCA were subjected for topographic, micromeritic, mechanical, compressional, and drug release properties.

Results: The process yielded ~92 to 98% wt/wt CCA containing secnidazole with the diameter between 0.2 and 0.7 mm. CCA showed excellent flow, packability, compatibility, and crushing strength. Heckel plot showed lower σ₀ and higher tensile strength with lower elastic recovery (0.55–1.28%) of CCA. Dissolution profile of CCA was improved. Differential scanning calorimetry , fourier transform infra-red, and x-ray diffractometry results showed absence of drug–excipient interaction.

Discussion: Matrix beads were generated with uniform dispersion of crystallized drug. Excellent flow, packability, and compactability were due to sphericity of agglomerates. Higher crushing strength of CCA was an indication of good handling qualities. Lower σ ₀, higher tensile strength, and lower elastic recovery indicated excellent compressibility of agglomerates. Improvement in dissolution profile was due to porous nature of CCA.

Conclusion: Excipients and polymers can play a key role to prepare CCA, an excellent alternative to wet granulation process to prepare particles for direct compression.     

Preparation and evaluation of poly(lactic-co-glycolic acid) microparticles as a carrier for pulmonary delivery of recombinant human interleukin-2: II. In vitro studies on aerodynamic properties of dry powder inhaler formulations

Objective: The aim of this study was the preparation and evaluation of dry powder formulations of recombinant human interleukin-2 (rhIL-2)-loaded microparticles to be administered to the lung by inhalation.

Methods: As indicated in our previous study, the microparticles were prepared by modified water-in-oil-in-water (w₁/o/w₃) double emulsion solvent extraction method using poly(lactic-co-glycolic acid) (PLGA) polymers. The dry powder formulations were prepared with blending of microparticles and mannitol as a coarse carrier. The actual aerodynamic characteristics of the microparticles alone and prepared mixtures with mannitol are evaluated by using the eight-stage Andersen cascade impactor.

Results: Due to the low tapped density of microparticles (<0.4?g/cm³), the theoretical aerodynamic diameter (MMADt) values were calculated (<5 μm) on the basis of the geometrical particle diameter and tapped density values. The lowest tapped density value (0.17?g/cm³) belongs to the cyclodextrin-containing formulation. According to the results obtained using the cascade impactor, the emitted doses for all microparticle formulations were found to be rather high and during the aerosolization for all the formulations except F3 and F5, >90% of the capsule content was determined to be released. However, the actual aerodynamic diameter (MMADa) values were seen to be higher than the MMADt values. The blending of the microparticles with mannitol allowed their aerodynamic diameters to decrease and their fine particle fraction values to increase.

Conclusion: The obtained results have shown that the mixing of rhIL-2-loaded microparticles with mannitol possess suitable aerodynamic characteristics to be administered to the lungs by inhalation.     

Characterization of agarose microparticles prepared by water-in-water emulsification

Microparticles have a wide range of applications in various areas. In this study, agarose microparticles (AGM) were successfully prepared by using a water-in-water (w/w) emulsification (WWEM) technique to eliminate the use of a surfactant. An aqueous agarose solution was employed as the dispersed phase, and polyethylene glycol (PEG) was used as the continuous phase. We evaluated how the characteristics of the microparticles were affected by different processing factors, including temperature, agitation speed, stirring time, concentration of agarose, and proportions of the two phases. The agarose microparticles obtained were nearly perfect spheres, and their particle sizes decreased with an increase in the agitation speed. Physicochemical characterization suggested that agarose microparticles, due to their ubiquitous stability, could be applied in most mild environments.     

Design and development of SMEDDS for colon-specific drug delivery

Abstract

Context: Lipoidal systems have particularly shown potential for specific accumulation in areas with inflamed tissue increasing the selectivity of local drug delivery.

Objective: Formulation and evaluation of self-microemulsifying drug delivery system (SMEDDS) for colon-specific drug delivery for effective treatment of colonic diseases.

Method: Ternary phase diagram was used to optimize level of oil, surfactant and co-surfactant to optimize SMEDDS and were evaluated for percent transmittance, emulsification time, in vitro release, myeloperoxidase (MPO) activity and intestinal accumulation. The spray dried SMEDDS were filled in capsules which were enteric coated with Eudragit S-100 at 10% weight gain to ensure SMEDDS delivery at colon. The spray dried SMEDDS were also evaluated for IR, DSC, XRD, SEM and stability study.

Result: In ternary phase diagram, Capmul MCM C8 and Capmul PG12 NF with surfactant (Tween 20) and co-surfactant (PG) in ratio 2:1 and 3:1, respectively, showed maximum emulsification area. These liquid SMEDDS show maximum transmittance, globule size of 90–30?nm. The spray-dried SMEDDS with diluents show good flow property. The units of MPO activity show lower level as compared to pure drug and control group, histopathology results supports better healing with SMEDDS. This was attributed to accumulation of SMEDDS in inflammatory area as compared to drug which was further proved by accumulation study. Enteric-coated capsule containing SMEDDS are able to deliver drug, specifically at the colonic region.

Conclusion: Higher accumulation of lipoidal drug in inflammatory area and specific release of liposomes by enteric-coated capsules provide better option for the treatment of colonic disease.     

Evaluation of Chlorpheniramine Maleate microparticles in orally disintegrating film and orally disintegrating tablet for pediatrics

Objective: To mask the bitterness of Chlorpheniramine Maleate via encapsulating drug into Eudragit EPO microparticles, and then incorporate these microparticles into orally disintegrating films (ODF) and orally disintegrating tablets (ODT) for pediatric uses.

Methods: Spray drying of water-in-oil emulsion was utilized to encapsulate Chlorpheniramine Maleate into Eudragit EPO microparticles. Based on an orthogonal experimental design L₉ (3³), polynomial regression models were developed to evaluate correlation between microparticle properties (encapsulation efficiency and drug release) and variables (X₁: weight ratio of polymer to drug, X₂: volume ratio of oil to water and X₃: Q-flow of spray dryer). ODF and ODT formulations were evaluated including weight variation, content uniformity, tensile strength, disintegration time, friability and dissolution profiles. The bitterness taste test was evaluated in 10 adult volunteers.

Results and discussion: From polynomial regression analysis, the best values of variables leading to the optimized microparticles were X₁?=?10, X₂?=?3 and X₃?=?45. The optimized microparticles were incorporated into ODF and ODT with satisfactory weight and drug content uniformity, and acceptable physical strength. Both dosage forms disintegrated immediately (less than 40?s) in simulated saliva solutions. The outcome of taste-masking test indicated that microparticles alleviated drug bitterness significantly; bitterness was not discernible with microparticles incorporated in ODT, whereas only slight bitterness was detected from microparticles incorporated into ODF.

Conclusion: Both ODF and ODT are shown to be suitable vehicles for taste masked Chlorpheniramine Maleate microparticles with potential for pediatric uses.