The effect of biomaterials of cross carmellose sodium and Eudragit S-100 as model polymers on colon targeted drug release in different dosage forms

The aim of the study was to prepare site specific drug delivery of naproxen sodium using sodium alginate and Eudragit S-100 as a mucoadhesive and pH-sensitive polymer, respectively. Core microspheres of alginate were prepared by a modified emulsification method followed by cross-linking with CaCl2, which was further coated with the pH dependent polymer Eudragit S-100 (2.5 or 5 %) to prevent drug release in the upper gastrointestinal environment. Microspheres were characterized by FT-IR spectroscopy, X-ray diffraction, differential scanning calorimetry and evaluated by scanning electron microscopy, particle size analysis, drug loading efficiency, in vitro mucoadhesive time study and in vitro drug release study in different simulated gastric fluids. Stability studies of the optimized formulation were carried out for 6 months. SEM images revealed that the surface morphology was rough and smooth for core and coated microspheres, respectively. Core microspheres showed better mucoadhesion compared to coated microspheres when applied to the mucosal surface of freshly excised goat colon. The optimized batch of core microspheres and coated microspheres exhibited 98.42 ± 0.96 and 95.58 ± 0.74 % drug release, respectively. Drug release from all sodium alginate microsphere formulations followed Higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the Korsmeyer-Peppas equation with a Fickian kinetics mechanism. Stability study suggested that the degradation rate constant of microspheres was minimal, indicating 2 years shelf life of the formulation.

Download Full-text

Design, Development, and Optimization of Polymeric Based-Colonic Drug Delivery System of Naproxen

The Scientific World JOURNAL ◽

10.1155/2013/654829 ◽

2013 ◽

Vol 2013 ◽

pp. 1-12 ◽

Cited By ~ 5

Author(s):

Pooja Sharma ◽

Anuj Chawla ◽

Pravin Pawar

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Ph Sensitive ◽

Time Dependent ◽

Wet Granulation ◽

Design Development ◽

Caecal Content ◽

S 100 ◽

Eudragit S 100

The aim of present investigation deals with the development of time-dependent and pH sensitive press-coated tablets for colon specific drug delivery of naproxen. The core tablets were prepared by wet granulation method then press coated with hydroxypropyl cellulose (HPC) or Eudragit RSPO : RLPO mixture and further coated with Eudragit S-100 by dip immerse method. Thein vitrodrug release study was conducted in different dissolution media such as pH 1.2, 6.8, and 7.4 with or without rat caecal content to simulate GIT conditions. Surface morphology and cross-sectional view of the tablets were visualized by scanning electron microscopy (SEM). All prepared batches were in compliance with the pharmacopoeial standards. The tablets which are compression coated with HPC followed by Eudragit S-100 coated showed highestin vitrodrug release of 98.10% in presence of rat caecal content. The SEM of tablets suggested that the number of pores got increased in pH 7.4 medium followed by dissolution of coating layer. The tablets coat erosion study suggested that the lag time depends upon the coating concentrations of polymers. A time-dependent hydrophilic polymer and pH sensitive polymer based press-coated tablets of naproxen were promising delivery for colon targeting.

Download Full-text

DESIGN AND EVALUATION OF EUDRAGIT COATED LOSARTAN POTASSIUM CONTROLLED RELEASE PELLETS BY PAN COATING TECHNIQUE

INDIAN DRUGS ◽

10.53879/id.50.10.p0030 ◽

2013 ◽

Vol 50 (10) ◽

pp. 30-38

Author(s):

S Vidyadhara ◽

◽

R. L. C. Sasidhar ◽

P Thrilochani ◽

L. K. Lavanya

Keyword(s):

Controlled Release ◽

Drug Release ◽

Methyl Cellulose ◽

Losartan Potassium ◽

Scanning Calorimetry ◽

Coating Agent ◽

Coating Technique ◽

S 100 ◽

Eudragit S 100

The present investigation was focused on the development and evaluation of controlled release pellets of losartan potassium with Eudragit S 100 and hydroxypropyl methyl cellulose phthalate (HPMCP) by employing pan coating technique. Eudragit S 100, a high viscosity grade controlled release polymer, was mainly used as coating agent for regulating the drug release from pellets. HPMCP, an enteric coating polymer was used in the present study to regulate the drug release at varied G.I. pH conditions. The prepared pellets were evaluated for particle size, drug content, friability and for in vitro drug release. The formulations were further characterized to identify any possible interactions by FTIR spectroscopy and differential scanning calorimetry. The surface morphology of the pellets was studied by scanning electron microscopy. From the results it was observed that due to increase in the concentration of Eudragit the drug release was extended up to 12 hours. The increase in the HPMCP polymeric concentration in formulations showed initial delay in drug release.

Download Full-text

Formulation and in vitro Assessment of Eudragit L 100 and Eudragit S 100 Based Naproxen Microspheres

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v15i1.29192 ◽

2016 ◽

Vol 15 (1) ◽

pp. 47-55

Author(s):

Md Ataur Rahman ◽

Nusrat Ahmed ◽

Ikramul Hasan ◽

Md Selim Reza

Keyword(s):

Particle Size ◽

Drug Release ◽

Release Kinetics ◽

Entrapment Efficiency ◽

Product Yield ◽

Drug Content ◽

S 100 ◽

Emulsification Solvent Evaporation ◽

Eudragit S 100

In the present study naproxen loaded microspheres were prepared by emulsification solvent evaporation method in order to achieve targeted drug delivery. Eudragit L 100 and Eudragit S 100 were used as the rate retardant polymers in the preparations. Thirteen formulations (F1-F13) were prepared using 22 factorial design by changing the concentration of these two polymers. All the formulations were evaluated for product yield, drug content, entrapment efficiency, particle size and drug release profiles. Highest drug content and entrapment efficiency were found to be 30.17% (F4) and 91.86% (F8) respectively. The particle size was found to be 159.26-234.70 ?m for all formulations. In-vitro drug release studies were performed using USP type II (Paddle) apparatus for 8 hrs in pH 7.4 phosphate buffer. The maximum drug release after 8 hrs was found to be 60.19% for batch F4. The release kinetics of all formulations were evaluated by using zero order, first order, Higuchi, Korsmeyer-Peppas, Kopcha and Hixson Crowell model. Almost all formulations fitted best with the Kopcha kinetic model. The SEM study indicated the spherical structure of the microspheres having rough surfaces.Dhaka Univ. J. Pharm. Sci. 15(1): 47-55, 2016 (June)

Download Full-text

Formulation and in vitro evaluation of Eudragit S-100 coated naproxen matrix tablets for colon-targeted drug delivery system

Journal of Advanced Pharmaceutical Technology amp Research ◽

10.4103/2231-4040.107498 ◽

2013 ◽

Vol 4 (1) ◽

pp. 31 ◽

Cited By ~ 26

Author(s):

Pravin Pawar ◽

Pooja Sharma ◽

Anuj Chawla ◽

Rohit Mehta

Keyword(s):

Drug Delivery ◽

Drug Delivery System ◽

Delivery System ◽

Targeted Drug Delivery ◽

Matrix Tablets ◽

S 100 ◽

Targeted Drug ◽

Eudragit S 100 ◽

Targeted Drug Delivery System

Download Full-text

DEVELOPMENT OF MESALAZINE MICROSPHERES FOR COLON TARGETING

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i4.17326 ◽

2017 ◽

Vol 9 (4) ◽

pp. 1

Author(s):

Katta Rajesh ◽

R. Deveswaran ◽

S. Bharath ◽

B. V. Basavaraj

Keyword(s):

Particle Size ◽

Drug Release ◽

Sustained Delivery ◽

Scanning Calorimetry ◽

Fourier Transformed Infrared Spectroscopy ◽

Aqueous Solvent ◽

S 100 ◽

Span 80 ◽

Eudragit S 100

Objective: The present work was aimed at preparation of mesalazine microspheres by a non-aqueous solvent evaporation method using eudragit S 100 and eudragit L 100 as pH dependent polymers for colon targeting.Methods: The ratio of drug to polymer was varied and the effect of formulation variables revolutions per minute (RPM) (1000, 1500, 2000 and 2500) and concentration of span 80 (1%, 1.5%, 2% and 2.5%) were studied. Prepared microspheres were evaluated for particle size, percent drug entrapment, granular analysis, in vitro drug release studies, Fourier transformed infrared spectroscopy (FT-IR) Differential Scanning Calorimetry (DSC), X-ray diffraction (XRD) and scanning electron microscopy (SEM) studies.Results: Particle size has decreased and percent drug entrapment had increased with increase in RPM in all formulations. When the span 80 concentration increased, the particle size of the microsphere formulations increased and percent drug entrapment decreased in eudragit S 100 microspheres; whereas in eudragit L 100 microspheres, as the concentration of span 80 increased, the particle size of the microsphere formulations decreased. The prepared microspheres sustained the drug release over a period of 12 h.Conclusion: Thus eudragit S 100 and eudragit L 100 microspheres could constitute a promising approach for colon-specific and sustained delivery of mesalazine for the treatment of inflammatory bowel disease.

Download Full-text

A NOVEL APPROACH OF LOCUST BEAN GUM MICROSPHERES FOR COLONIC DELIVERY OF MESALAMINE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2018v10i1.22638 ◽

2018 ◽

Vol 10 (1) ◽

pp. 86 ◽

Cited By ~ 1

Author(s):

V. N.l. Sirisha ◽

M. Chinna Eswariah ◽

A. Sambasiva Rao

Keyword(s):

Drug Release ◽

Entrapment Efficiency ◽

Locust Bean Gum ◽

Ionic Gelation ◽

Stability Studies ◽

In Vitro Drug Release ◽

S 100 ◽

Locust Bean ◽

Eudragit S 100

Objective: The objective of the present study was to formulate site-specific drug delivery of mesalamine using Locust bean gum.Methods: The core microspheres were prepared by ionic gelation method using CaCl2 solution and cross-linked with glutaraldehyde and were further coated with pH-sensitive polymer eudragit S-100(1.5-4.5 ml) to retard the drug release in the upper gastrointestinal environment (Stomach and small intestine). Microspheres were characterized by ftir spectroscopy, differential scanning calorimetry and evaluated by scanning electron microscopy (SEM), particle size analysis, entrapment efficiency and in vitro drug release studies in different simulated gastric fluids. Stability studies were carried out for one month at 40±2 °C/75±5% RH.Results: The SEM images revealed the surface morphology was rough and smooth for core and coated microspheres, respectively. The optimized batch (ILBG6) of core microspheres(for 7hr), coated microspheres and coated microspheres in presence of rat caecal contents (8%w/v) for 24hr exhibited 98.44±2.48, 73.58±3.49 % and 98.28±4.42 drug release, respectively. The drug release from all locust bean gum microsphere formulations followed higuchi kinetics. Moreover, drug release from Eudragit S-100 coated microspheres followed the korsmeyer-peppas equation with an fickian kinetics mechanism. Finally, stability studies suggested the change in entrapment efficiency and in vitro drug release of microspheres was minimal, indicating good stability of the formulation.Conclusion: The microspheres formed using natural polysaccharide locust beangum by ionic gelation method are capable of colon targeting the anti-inflammatory drug, mesalamine for the treatment of ulcerative colitis.

Download Full-text