QbD-Enabled Systematic Development of Ileo-colonic Targeted Novel Mucoadhesive Microspheres of Flurbiprofen

2021 ◽  
Vol 18 ◽  
Author(s):  
Saikat Pande ◽  
Janu Vashi ◽  
Ajay Solanki
Keyword(s):  
Ulcerative Colitis ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Sem Analysis ◽  
Release Profile ◽  
Chitosan Microspheres ◽  
S 100 ◽  
Ft Ir ◽  
Full Factorial ◽  
Eudragit S 100

Background: Flurbiprofen (FLBP) is used in the treatment of ulcerative colitis and has a short biological half-life. Frequent intake of FLBP may lead to some serious gastric complications, which makes FLBP an ideal candidate for sustained release preparation to the Ileo-colonic region of the gastrointestinal tract (GIT). Objective: The objective of this study was to investigate the potential of Eudragit coated chitosan microspheres in delivering Flurbiprofen in a sustained manner to the Ileo-colonic region of the GIT for treatment of ulcerative colitis. Methods: In the present study, mucoadhesive chitosan microspheres were prepared using the emulsion solvent evaporation method by varying different process parameters. Optimized chitosan microspheres were coated with Eudragit L-100 and Eudragit S-100. A 32 full factorial design was applied for optimization. The effect of independent variables (Eudragit L-100 to Eudragit S-100 ratio and stirring speed) on the dependent variable, i.e., percentage cumulative drug release (%CDR) at 3 h and 24 h was evaluated. The optimized batch was evaluated by FT-IR, DSC study, XRD study, and SEM analysis. Results: Discrete spherical shape chitosan microspheres with entrapment efficiency of up to 95.4% were obtained and selected for coating. Chitosan microspheres coated successfully with different ratios of Eudragit L-100 to Eudragit S-100. The release profile of the optimized batch match with the desired release profile. FLBP was found to be stable and molecularly dispersed in the polymer matrix. Conclusion: Taken together, it can be concluded that prepared microspheres may be considered suitable for delivering FLBP to the Ileo-colonic region of the GIT in the treatment of ulcerative colitis.

Formulation and Evaluation of Mucoadhesive Floating Microspheres of Repaglinide

2021 ◽  
pp. 5673-5679
Author(s):  
S. Sivaprasad ◽  
V. Alagarsamy ◽  
M. Prathibha Bharathi ◽  
P.V. Murali Krishna ◽  
K. Sandeeep Kanna
Keyword(s):  
Controlled Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Extended Period ◽  
Entrapment Efficiency ◽  
Sustain Release ◽  
S 100 ◽  
Eudragit S 100 ◽  
Good Flow

The main objective of the present study was to design a controlled release dosage form for an oral anti diabetic drug i.e. repaglinide employing polymers like eudragit s- 100. One of the other objective of this present study was to increase the biological half-life the drug by formulating into microspheres. The microspheres of repaglinide were prepared by solvent evaporation method by using eudragit s-100 and ethyl cellulose as polymers with different concentrations. Formulations (F1-F10) were prepared and evaluated for various micrometric properties and it was observed that though all the formulations were exhibited good flow properties, The F5 formulation exhibits higher in- vitro buoyancy time and entrapment efficiency which is considered for in- vitro and mucoadhesive studies. The FTIR results reveal that there was no interaction between the drug and the excipients. The in- vitro release profiles of F1-F5 indicated that all formulations showed controlled release over an extended period, with acceptable release kinetics. Among the all formulations F5 were considered as a promising candidate for sustain release of repaglinide.

scholarly journals Entacapone – Based Floating Microspheres by Ionotropic Gelation Technique-Morphology and Release Characteristics

2018 ◽  
Vol 10 (02) ◽  
Author(s):  
Suggala Ajay ◽  
Gande Suresh
Keyword(s):  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Sem Analysis ◽  
Potential Candidate ◽  
Ionotropic Gelation ◽  
Gastric Residence Time ◽  
Sustained Drug Delivery ◽  
Diffusion Studies ◽  
Gastro Retentive

The main objective of the present investigation was to develop gastro retentive floating microspheres for Entacapone. These are prepared by ionotropic gelation method with an aim of increasing the gastric residence time and for controlled release. The polymeric mixture of Sodium alginate and HPMC K4, was used as polymers. Sodium bicarbonate was used as the gas-forming gent. Prepared Microspheres were characterized for the Micromeretic properties, incorporation efficiency, buoyancy test, SEM analysis, FTIR, and in vitro diffusion studies. The diffusion studies were carried out in 0.1N HCl and the results were applied to various kinetic models. Among the total 14 formulations F14 was optimized. The % yield of F14 formulation was found to be 98.03%. Based on optical microscopy, the particle size was 65.23 ± 0.05μm. The % buoyancy, % entrapment efficiency and swelling index of F14 formulation was 98.16%, 97.54% and 97.67%, respectively. The cumulative % drug release of F14 formulation was 97.99 ± 5.05% in 12 h when compared with marketed product 95.12 ± 5.01 in 1 h. SEM studies showed the particles were in spherical shape. Hence the formulated and prepared floating Entacapone microspheres may establish to be potential candidate for safe and effective sustained drug delivery and improve the bioavailability in the management of Parkinson’s disease.

Design, Formulation and Characterization of Microspheres containing Mesalamine for the Treatment of Ulcerative Colitis

2021 ◽  
pp. 165-169
Author(s):  
Deepak Patel ◽  
Sunil Kumar Shah ◽  
Chandra Kishore Tyagi
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Simulated Gastric Fluid ◽  
Simulated Intestinal Fluid ◽  
Chitosan Microspheres ◽  
Increase With Increase

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72% - 82.27%, drug loading from 20.28% - 33.26%. The size of the prepared microspheres ranged between 61.22-90.41μm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. The release profile of mesalamine from eudragit-coated chitosan micro-spheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.

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

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)

scholarly journals Nizatidine Based Floating Microspheres by Ionotropic Gelation Technique - Morphology and Release Characteristics

2018 ◽  
Vol 10 (03) ◽  
Author(s):  
D.V. R. N. Bhikshapathi ◽  
U. Ashok Kumar, ◽  
A. Shylaja Rani
Keyword(s):  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Sem Analysis ◽  
In Vitro Dissolution ◽  
H2 Receptor Antagonist ◽  
Histamine H2 Receptor ◽  
Ulcer Disease ◽  
Ionotropic Gelation ◽  
Dissolution Studies

Nizatidine is a histamine H2-receptor antagonist that inhibits stomach acid production and used in the treatment of peptic ulcer disease and gastroesophageal reflux disease. The main aim of the present investigation was to develop gastro retentive floating microspheres for Nizatidine. These are prepared by ionotropic gelation method with an aim of increasing the gastric residence time and for controlled release. The polymeric mixture of Sodium alginate and HPMCK4, HPMC K15M and HPMC K 100M, was used as polymers. Calcium carbonate was used as the gas forming gent. Prepared Microspheres were characterized for the Micromeretic properties, incorporation efficiency, buoyancy test, SEM analysis, FTIR, and in vitro dissolution studies. The dissolution studies were carried out in 0.1N HCl and the results were applied to various kinetic models. Among the total 18 formulations F17 was optimized. The % yield of F17 formulation was found to be 95.47 ± 0.36%. Based on optical microscopy, the particle size was 50.67 ± 0.13μm. The % buoyancy, % entrapment efficiency and swelling index of F17 formulation was 94.23%, 93.62 ± 0.29% and 92.13 ± 0.17%, respectively. The Cumulative % drug release of F17 formulation was 98.23 ± 5.49% in 12 h when compared with marketed product 95.87 ± 0.31 in 12 h. SEM studies showed the particles were in spherical shape. Based on obtained results, Floating alginate Nizatidine microspheres were of good candidate for targeting to GIT.

Eudragit S-100 entrapped chitosan microspheres of valdecoxib for colon cancer

2010 ◽  
Vol 21 (9) ◽  
pp. 2691-2699 ◽  
Author(s):  
Naveen K. Thakral ◽  
Alok R. Ray ◽  
Dipak K. Majumdar
Keyword(s):  
Colon Cancer ◽  
Chitosan Microspheres ◽  
S 100 ◽  
Eudragit S 100

scholarly journals Development and Evaluation of Sustained Release Floating Microspheres Containing Ropinirole HCl

2018 ◽  
Vol 10 (03) ◽  
Author(s):  
Koppula Subbarao ◽  
Gande Suresh
Keyword(s):  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Sem Analysis ◽  
In Vitro Dissolution ◽  
Potential Candidate ◽  
Gastric Residence Time ◽  
Sustained Drug Delivery ◽  
Evaluation Parameters ◽  
Gastro Retentive

Current investigation was to develop gastro retentive floating microsphere for Ropinirole. These microspheres of Ropinirole were prepared by ionic gelation method with an aim of increasing the gastric residence time and for controlled release. Sodium alginate, HPMCK15, Gaur gum was used as polymers. Sodium bicarbonate was used as the gas-forming gent. Prepared microspheres were characterized for micromeretic properties, entrapment efficiency, buoyancy study, SEM analysis, FTIR, and in vitro dissolution studies. Among 14 formulations F12 was found to be optimized and based on the evaluation parameters. The % buoyancy, % yield, % entrapment efficiency and swelling index of F12 formulation was 94.50, 97.58, 98.10% and 96.14%, respectively. The Cumulative % drug release of F12 formulation was 98.16 ± 5.15 in 12 h when compared with marketed product 90.16 ± 5.00 in 12 h. SEM studies showed the particles were in spherical shape. Hence the formulated floating Ropinirole microspheres may establish to be potential candidate for safe and effective sustained drug delivery and improve the bioavailability in the effective management of Parkinson’s disease.

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

2018 ◽  
Vol 10 (1) ◽  
pp. 86 ◽  
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.

scholarly journals Colon specific drug delivery of mesalamine using eudragit S100-coated chitosan microspheres for the treatment of ulcerative colitis

2013 ◽  
Vol 2 (3) ◽  
pp. 42-48 ◽  
Author(s):  
Seema Badhana ◽  
Navneet Garud ◽  
Akanksha Garud
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Targeted Delivery ◽  
Drug Loading ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
Simulated Gastric Fluid ◽  
Chitosan Microspheres ◽  
Increase With Increase ◽  
Eudragit S100

The purpose of the present study was to prepare, characterize and evaluate the colon-targeted microspheres of mesalamine for the treatment and management of ulcerative colitis (UC). Microspheres were prepared by the ionic-gelation emulsification method using tripolyphosphate (TPP) as cross linking agent. The microspheres were coated with Eudragit S-100 by the solvent evaporation technique to prevent drug release in the stomach. The prepared microspheres were evaluated for surface morphology, entrapment efficiency, drug loading, micromeritic properties and in-vitro drug release. The microspheres formed had rough surface as observed in scanning electron microscopy. The entrapment efficiency of microspheres ranged from 43.72%-82.27%, drug loading from 20.28%-33.26%. The size of the prepared microspheres ranged between 61.22-90.41µm which was found to increase with increase in polymer concentration. All values are statistically significant as p<0.05. Micromeritic properties showed good flow properties and packability of prepared microspheres. The drug release of mesalamine from microspheres was found to decrease as the polymer concentration increases. The release profile of mesalamine from eudragit-coated chitosan microspheres was found to be pH dependent. It was observed that Eudragit S100 coated chitosan microspheres gave no release in the simulated gastric fluid, negligible release in the simulated intestinal fluid and maximum release in the colonic environment. It was concluded from the study that Eudragit-coated chitosan microspheres were promising carriers for colon-targeted delivery of Mesalamine.DOI: http://dx.doi.org/10.3329/icpj.v2i3.13577 International Current Pharmaceutical Journal, February 2013, 2(3): 42-48 

Formulation and Characterization of Losartan Loaded Chitosan Microspheres: Effect of Crosslinking Agents

Drug Research ◽  
2020 ◽  
Author(s):  
Sonia Pahuja ◽  
Shweta Aggarwal ◽  
Prerna Sarup
Keyword(s):  
Average Particle Size ◽  
In Vitro Release ◽  
Spherical Shape ◽  
Entrapment Efficiency ◽  
Cross Linking ◽  
Average Particle ◽  
Chitosan Microspheres ◽  
Optimum Parameters ◽  
Sustained Effect

Abstract Objective The present investigation entailed determination of effect of diverse cross-linking agents on Losartan Potassium loaded chitosan microspheres. The emulsion cross-linking method was employed to formulate the microspheres with an endeavour to achieve maximum sustained effect. Methods The FTIR studies revealed absence of any interaction between Losartan and chitosan. The emulsion cross linking method was accomplished in three steps encompassing formation of an aqueous and oily phase, emulsification and cross-linking. A total of eighteen Losartan formulations were developed using six different cross-linkers at three varying level were screened for optimum parameters. The in vitro drug release parameters of optimum formulations (LC3, LE3, LF3, LG3, LS3 and LV3) containing citric acid, epichlorohydrin, formaldehyde, glutaraldehyde, suphuric acid and vanillin as cross-linkers were assessed to determine the sustained effect. Results The values of evaluated parameters including percent yield (94.67%), average particle size (51.19 µm), drug content (44.38 mg) and entrapment efficiency (88.77%) connoted LG3 as the best formulation. Additionally, the values of relative measure of skewness (β1=0.01 and γ1=0.10) and platykurtic (β2=1.26) size distribution were least for LG3 with spherical shape and smooth surface as revealed by SEM studies. Conclusion The outcome of in vitro release and other characterizations of microspheres explicitly revealed glutaraldehyde as the best cross-linker amongst the cross-linkers used herewith. The maximum sustained effect (lasting over a period of 24 h) accompanied with higher MDT and t50% with lower%DE and Q14h values thus corroborated the objective of attaining sustained release of Losartan.

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