scholarly journals QBD-BASED DEVELOPMENT AND EVALUATION OF ENTERIC COATED MUCOADHESIVE MICROCAPSULES OF AMOXICILLIN TRIHYDRATE AS A NOVEL CHRONOTHERAPEUTIC APPROACH FOR TREATMENT OF BACTERIAL INFECTIONS

2018 ◽  
Vol 10 (8) ◽  
pp. 90 ◽  
Author(s):  
Shyam Narayan Prasad ◽  
Hemant Kumar Patel ◽  
Abhijit V. Gothoskar
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Entrapment Efficiency ◽  
Drug Content ◽  
Eudragit L100 ◽  
Significant Difference ◽  
Amoxicillin Trihydrate ◽  
Mucoadhesive Property ◽  
Enteric Coated

Objective: The present work entails design and characterization of enteric coated mucoadhesive microcapsules loaded with amoxicillin trihydrate as a novel chronotherapeutic approaches for the treatment and management of bacterial infection.Methods: The microcapsules were prepared by solvent evaporation technique using ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) as rate-controlling and mucoadhesive polymers, followed by a triple coating with Eudragit L100 as enteric coating polymer. Box-Behnken statistical design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The optimized microcapsules were also characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity.Results: The optimized microcapsules exhibited good entrapment efficiency, particle size and mucoadhesive property. FT-IR studies revealed that there was no drug-polymer interaction. SEM studies revealed that microcapsules were non-aggregated, spherical in shape and smooth appearance. In vitro drug release data from microcapsules was fitted to different kinetic models to explain release profiles. The correlation coefficient (r2) value indicated that drug release followed Higuchi model. Analysis of variance (ANOVA) showed significant difference in the release of drug from all the prepared formulations at P < 0.05 level. Accelerated stability study of optimized formulation (F4) upto 6 month showed there was no change in drug content and release characteristics during storage.

scholarly journals FORMULATION OF POLYMERIC NANOSUSPENSION CONTAINING PRAMIPEXOLE DIHYDROCHLORIDE AND HESPERIDIN FOR IMPROVED TREATMENT OF PARKINSON’S DISEASES

2018 ◽  
Vol 11 ◽  
Author(s):  
Somasundaram I
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Burst Release ◽  
Drug Content ◽  
Pramipexole Dihydrochloride ◽  
Vitro Release

Aims and Objectives: The present study is to formulate the nanosuspension containing a hydrophilic drug pramipexole dihydrochloride and hesperidin and to increase the drug entrapment efficiency.Methods: Hesperidin and pramipexole dihydrochloride loaded in chitosan nanosuspension is prepared by ionic gelation method using chitosan and tripolyphosphate. There was no incompatibility observed between the drug and polymer through Fourier transform infrared and differential scanning calorimetric. Various other parameters such as particle size, zeta potential, scanning electron microscope, drug content, drug entrapment efficiency, and in vitro release have been utilized for the characterization of nanoparticles.Results and Discussion: The average size of particle is 188 nm; zeta potential is 46.7 mV; drug content of 0.364±0.25 mg/ml; entrapment efficiency of 72.8% is obtained with HPN3 formulation. The PHC1 shows the highest drug release followed by PHC2 due to low concentration of polymer and PHC4 and PHC5 show less drug release due to high concentration of polymer. The in vitro release of PHC3 is 85.2%, initial the burst release is shown which is approximately 60% in 8 h; then, slow release later on drastic reduction in release rate is shown in 24 h. The in vivo study histopathological report confers the effective protective against rotenone induces Parkinson’s.Conclusion: PHC3 was chosen as the best formulation due to its reduced particle size and controlled release at optimum polymer concentration which may be used to treat Parkinson’s disease effectively..

scholarly journals Oral Formulation of Anticancer Agents for Colon Cancer

2021 ◽  
pp. 402-418
Author(s):  
Dipti Patel ◽  
Krishna Patel
Keyword(s):  
Colon Cancer ◽  
Particle Size ◽  
Anticancer Agents ◽  
Crosslinking Agent ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Inlet Temperature ◽  
Disintegration Time ◽  
Drug Content ◽  
Enteric Coated

Aims/Objective: To develop and estimate enteric-coated capsules containing mucoadhesive Microspheres of Capecitabine and Oxaliplatin to treat Colon cancer. Study Design: Box Behnken. Place and Duration of Study: Department of Pharmaceutics, Parul Institute of Pharmacy and Research, Parul University, Vadodara, between 2017 to 2021. Methodology: Capecitabine and Oxaliplatin are used as antineoplastic agents and can be delivered via the oral route of administration. For the estimation of drugs Analytical method has been developed by HPLC. Box Behnken design has been used to optimize Drug: polymer ratio (1:2), Inlet temperature 170ºC, and crosslinking agent with a 0.5 ml 1% Gluteraldehyde solution. The microspheres were successfully prepared by using the spray drying technique and evaluated. Results: The results of optimized Capecitabine microspheres were obtained as Particle size 87.91 µm ± 0.274,% yield 57.21± 1.5,% Mucoadhesion 57.21± 1.5,% entrapment efficiency 82.16± 0.725. The results of optimized Oxaliplatin microspheres were obtained as Particle size 99.88µm±0.034,% yield 56.0± 0.088,% Mucoadhesion 87.0± 0.80,% entrapment efficiency 82.61±0.085. The drug content of Capecitabine and Oxaliplatin in the filled capsule was 94.67% ±0.32 and 93.45%±0.712, respectively. % Drug release of Capecitabine and Oxaliplatin in Phosphate buffer pH 7.4 was found to be 94.83±0.22 and 96.94±0.11 respectively after 8 hrs. Stability study at 400C±20C / 75 ± 5 % RH revealed that there was no significant change in disintegration time, drug content and % CDR during 6 months. So, prepared formulation was stable during stability study.  MTT assay has been performed on the formulation of Capecitabine and Oxaliplatin microspheres for assessing the % viability of both the drugs on the Caco-2 cell line. Conclusion: The present study confirmed that prepared mucoadhesive microspheres filled with enteric-coated capsules have an antitumor effect on colon cancer cells. The formulation induced high cell death within 48 hours, and less cell viability was obtained compared to API. Six months accelerated Stability study indicates that formulation is fairly stable at storage conditions.

Design and Development of Lomustine Loaded Chitosan Nanoparticles for Efficient Brain Targeting

2020 ◽  
Vol 18 (1) ◽  
pp. 45-54 ◽  
Author(s):  
Anupriya Anand ◽  
Bharadhwaj Ramesh Iyer ◽  
Chandrasekar Ponnusamy ◽  
Rajesh Pandiyan ◽  
Abimanyu Sugumaran
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Research Work ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Brain Targeting ◽  
P Value ◽  
Drug Content ◽  
Diffusion Controlled

Aim: The present research work discussed the preparation of lomustine loaded with chitosan nanoparticles (LNCp) by ionic gelation method with homogenization using the design on experiments by Box-Behnken design. Methods: The nanoparticles are evaluated by particle size, zeta potential, surface morphology, drug content, entrapment efficiency and in-vitro drug release. Results: The FT-IR results support that drug have no interaction with excipients, which are used in the preparation of nanoparticle. The particle size, drug content and encapsulation efficiency of the developed nanoparticles ranged from 190 to 255 nm, 80.88% to 94.02%, and 77.12 to 88.74%, respectively. The drug release rate is diffusion-controlled over 8 hours. The F-value for all of the responses shows that the models are significant. The p-value, less than 0.05 for all the responses reveals the significance of the models. Graphical optimisation is done by desirability plot and overlay plot, which contains optimal values of independent variables with the desirability of 1. Conclusion: In conclusion, the results suggested that the optimised lomustine loaded chitosan nanoparticles are useful for brain targeting hence hold the potential for further research and clinical application.

scholarly journals A NOVEL NANOGEL FORMULATION OF FINASTERIDE FOR TOPICAL TREATMENT OF ANDROGENETIC ALOPECIA: DESIGN, CHARACTERIZATION AND IN VITRO EVALUATION

2021 ◽  
pp. 228-240
Author(s):  
DIVYA SANGANABHATLA ◽  
R. SHYAM SUNDER
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Androgenetic Alopecia ◽  
Stability Studies ◽  
Drug Content ◽  
Release Study

Objective: The present paper describes the development and evaluation of a Novel Finasteride (FSD) nanogel topical delivery for the treatment of Androgenetic Alopecia. Nano-based topical formulation was chosen to enhance the solubility, permeability, biocompatibility of drug and to overcome the problems associated with the oral delivery of finasteride. Methods: Various trails batches were prepared by using probe sonication method. Based on stability studies and particle size, NP4 trail was optimized which exhibited a spherical shape with a mean diameter of 113.80±0.72, the polydispersity of 0.28±0.01, zeta potential of-25.2 mV, drug entrapment efficiency of 92.67±0.47 %, and drug loading of 6.15±0.02 %. Storage stability studies demonstrated that the particle size and entrapment efficiency were not changed during 3 mo both at 4 °C and room temperature. Finasteride (FSD) NLCs were characterized for particle size by scanning electron microscope (SEM), chemical state by X-Ray diffraction (XRD), physical stability by centrifugation and thermodynamic stability by Freeze-thaw method. These prepared nanoparticles were transformed into topical nanogel and further evaluated. Results: Among the different trails, C2 trail of NLC gel has shown excellent gelling capacity, clear appearance, good viscosity characteristics and was selected for further evaluation studies. Batches of topical nanogel were characterized through pH, homogeneity, spreadability, viscosity, drug content and in vitro drug release study. Based on pH (6.5-6.8), drug content (91.25±0.9%), spreadability (6.7 cm/sec), C2 batch was subjected to In vitro skin occlusivity study, in-vitro release study and In vitro heamolysis study. Conclusion: The percent cumulative drug release for Finasteride (FSD) gel was found to be 758.52±1.49 µg at 24 h which is quite higher than plain gel and Finasteride (FSD) gel showed maximum occlusiveness and excellent spreadability and found to be stable. In conclusion, prepared Finasteride (FSD) Nanogel could be used with promising potential for the treatment of Androgenetic Alopecia.

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 DEVELOPMENT AND CHARACTERIZATION OF DICLOFENAC SODIUM LOADED EUDRAGIT RS100 POLYMERIC MICROSPONGE INCORPORATED INTO IN SITU GEL FOR OPHTHALMIC DRUG DELIVERY SYSTEM

2021 ◽  
pp. 63-69
Author(s):  
RAJASHRI B. AMBIKAR ◽  
ASHOK V. BHOSALE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
In Situ Gel ◽  
Drug Content

Objective: Purpose of the study to design and formulate Diclofenac sodium (DIC) microsponges. Methods: With varied polymer: drug ratio DIC loaded microsponges were prepared with Eudragit RS100 polymer by quasi solvent diffusion method. Microsponges evaluated for particle size, entrapment efficiency, drug content, in vitro drug release, Fourier Transform Infrared Spectroscopy (FTIR), Differential scanning calorimetry (DSC) and Scanning electron microscopy (SEM). DIC loaded microsponges incorporated into ocular in situ gel to attained controlled release by microsponge and improved residence time by gelling system. Ocular in situ gel evaluated for pH, drug content determination, gelling capacity, in vitro drug release and sterility study. Results: DSER4 microsponge formulation having polymer to drug ratio 1:7 showed satisfactory production yield (68.13%), entrapment efficiency (62.86%), drug content (80.73%), requisite particle size (less than 10 µm) (7.52 µm) and in vitro release 87.94% after 6 h. Selected DSER4 formulation was incorporate into in situ gel. Carbopol 940 forms stiff gel at higher pH so used as a gelling agent, whereas Hydroxypropyl Methylcellulose E4M was used as a viscosity-enhancing agent for the formulation of in situ gel in varied compositions. In situ gel formulation IG4 showed sustained release of 76.92% till the end of 8 h and satisfactory gelling capacity so IG4 further evaluated for sterility test. Rheological studies reveal the sol-gel transition of in situ gel occur at the physiological condition to form stiff gel. Conclusion: Prepared in situ gel formulations showed sustained drug release for a period of 8 h, which is satisfactory for management of ocular pain.

scholarly journals Investigating The Retention Potential of Chitosan Nanoparticulate Gel: Design, Development, In Vitro & Ex Vivo Characterization

2020 ◽  
Vol 15 (1) ◽  
pp. 41-67
Author(s):  
Shreya Kaul ◽  
Neha Jain ◽  
Jaya Pandey ◽  
Upendra Nagaich
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ex Vivo ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Eye Drops ◽  
Design Development ◽  
In Vitro Drug Release ◽  
Drug Content

Introduction: The main purpose of the research was to develop, optimize and characterize tobramycin sulphate loaded chitosan nanoparticles based gel in order to ameliorate its therapeutic efficacy, precorneal residence time, stability, targeting and to provide controlled release of the drug. Methods: Box-Behnken design was used to optimize formulation by 3-factors (chitosan, STPP and tween 80) and 3-levels. Developed formulation was subjected for characterizations such as shape and surface morphology, zeta potential, particle size, in vitro drug release studies, entrapment efficiency of drug, visual inspection, pH, viscosity, spreadability, drug content, ex vivo transcorneal permeation studies, ocular tolerance test, antimicrobial studies, isotonicity evaluation and histopathology studies. Results: Based on the evaluation parameters, the optimized formulation showed a particle size of 43.85 ± 0.86 nm and entrapment efficiency 91.56% ± 1.04, PDI 0.254. Cumulative in vitro drug release was up to 92.21% ± 1.71 for 12 hours and drug content was found between 95.36% ± 1.25 to 98.8% ± 1.34. TEM analysis unfolded spherical shape of nanoparticles. TS loaded nanoparticulate gel exhibited significantly higher transcorneal permeation as well as bioadhesion when compared with marketed formulation. Ocular tolerance was evaluated by HET-CAM test and formulation was non-irritant and well-tolerated. Histopathology studies revealed that there was no evidence of damage to the normal structure of the goat cornea. As per ICH guidelines, stability studies were conducted and were subjected for 6 months. Conclusion: Results revealed that the developed formulation could be an ideal substitute for conventional eye drops for the treatment of bacterial keratitis.

scholarly journals BETAMETHASONE DIPROPIONATE GEL FOR TREATMENT OF LOCALIZED PLAQUE PSORIASIS

2017 ◽  
Vol 9 (8) ◽  
pp. 173 ◽  
Author(s):  
Sanaa El Gizaway ◽  
Maha Fadel ◽  
Basma Mourad ◽  
Fatma El-zahraa Abd Elnaby
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Betamethasone Dipropionate ◽  
Average Particle ◽  
Topical Formulation ◽  
Content Type ◽  
Drug Content

Objective: The main aim of this study was to design and characterise betamethasone di-propionate loaded transfersomes (BD-T); as a topical formulation for the treatment of localized plaque psoriasis.Methods: A full factorial design (23) was applied to study the effects of three independent variables: drug content, type of surfactants and surfactant contents on particle size (PS), entrapment efficiency (EE %), zeta potential (ZP), polydispersity index (PI) and drug release profiles. The optimized BD-T was formulated as a hydrogel using 5% sodium carboxymethyl cellulose. The gel was characterized for viscosity, drug content, in vitro drug release and stability. A comparative clinical study was performed on 20 patients with psoriasis to investigate the effect of BD-T gel and the marketed betamethasone dipropionate (BD) cream.Results: The optimized BD-T formulation containing 50 mg betamethasone dipropionate (BD) and 5 mg tween 80 showed spherical unilamellar vesicles with an average particle size of 242.80, % EE of 90.19%, ZP of-15.00 mV, PI of 0.407 and K0 of 4.290 mg/hr. The formulation showed good stability at 4 °C and 25 °C for 6 mo. The results revealed significant clinical improvement and a significant increase in safety and tolerability with BD-T gel compared with BD cream.Conclusion: As a conclusion, BD-T was found to be more effective, safe and tolerable for the treatment of psoriasis compared with the marketed product.

scholarly journals Formulation and Evaluation of Eudragit Rl100 Polymeric Drug Loaded Microsponge for Ophthalmic Use

2021 ◽  
pp. 45-51
Author(s):  
Rajashri B. Ambikar ◽  
Ashok V. Bhosale
Keyword(s):  
Particle Size ◽  
Controlled Release ◽  
Drug Release ◽  
Delivery System ◽  
Diffusion Mechanism ◽  
Diclofenac Sodium ◽  
Entrapment Efficiency ◽  
Fickian Diffusion ◽  
Drug Content

Aims: The aim of this work is the formulation of Eudragit RL100 polymeric microsponges. The Microsponge Delivery System is a patented technique in which there is a polymeric system consisting of porous particles. Methodology: The ratio of Diclofenac sodium and eudragit RL100 varied from 1:1 to 13: 1 to formulate microsponge. Dichloromethane was used as internal phase and polyvinylalcohol was used as an external phase. The formed microsponges were characterized for particle size, entrapment efficiency, drug content, in vitro drug release and SEM. Results: With increase in drug: polymer ratio there is increase in production yield from 20.04% to 72.14%, and entrapment efficiency from 20.11% to 70.77%.  Drug content of formed microsponge varied between 50.18% to 91.09% whereas particle size ranged from 1.41 µm to 17.66 µm. Microsponge formulations F3, F4 and F5 showed desired particle size hence studied for further evaluation. Formulation F3, F4 and F5 showed controlled release of 89.54%, 98.5% and 98.76% respectively up to 6 hr. F3 showed more controlled release at the end of 6 hr. The drug release from microsponges was best fitted to Higuchi’s diffusion kinetics for all microsponge formulations with non-Fickian diffusion mechanism. The formed microsponge particles have spherical porous structure. Conclusion: Study showed significance of Microsponge Delivery System for ophthalmic administration.

scholarly journals Formulation and in-vitro evaluation of Glipizide (Anti diabetic drug) Liposphere

2018 ◽  
Vol 8 (6-s) ◽  
pp. 116-119
Author(s):  
Sarika Saini ◽  
Aman Mittal
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
In Vitro Study ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Paraffin Wax ◽  
Drug Content ◽  
Dissolution Apparatus ◽  
Dispersion Technique

Objective- The aim of the present study was to formulate and in- vitro study of glipizide liposphere by using melt dispersion technique. Methods- Glipizide Liposphere system composed of paraffin wax, Stearic acid as lipid phase and sodium lauryl sulphate as surfactant. Glipizide lipospheres were prepared by using melt dispersion technique. Formulation of Glipizide was evaluated such as organoleptic properties, particle size, drug content, entrapment efficiency in-vitro study and stability of the lipospheres. Result- The formation of glipizide lipospheres by using melt dispersion technique was done successfully. All the formulations have off- white in colour, characteristic odour and spherical shape. The formulation A4 has particle size 19.65 μm, drug content 84.93 %, entrapment efficiency 80.75 % and the percentage drug release was carried out by using USP type 2 dissolution apparatus in 6.8 pH phosphate buffer solution and drug release of glipizide lipospheres within 12 hrs was found to be 74.06 %.stability study of glipizide lipospheres revealed that the formulation was stable at 5oC ± 3oC. Keywords- Lipospheres, Glipizide, Paraffin wax, Melt dispersion method, Dissolution Apparatus, Stability study

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