scholarly journals Formulation and evaluation of nanoparticulate ofloxacin ophthalmic gel using ionic gelation method

2019 ◽  
Vol 1 (2) ◽  
pp. 73-78
Author(s):  
B Syed Salman ◽  
Mohd Abdul Hannan Baig
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
In Vitro Drug Release ◽  
Entire Study ◽  
Drug Content ◽  
Higuchi Model

Oflaxacin is an ophthalmic and topical anti-bacterial agent used in the management of Allergic conjunctivitis, Trachoma, Blepharitis. The basic idea behind the development of such a system is to maintain a sustained drug release from the dosage form. Oflaxacin is suitable candidate for formulation into sustained dosage form in order to prolong the release of drug. The drug-excipient compatibility studies were carried out by using FTIR technique. Based on the results, excipients were found to be compatible with ofloxacin. In preformulation study, estimation of Ofloxacin was carried out by systronics UV spectrophotometer at λmax 284nm using distilled water, which had a good reproducibility and this method was used in entire study. Formulation was prepared by using ionic gelation method .The response drug content, entrapment efficiency, diffusion, spreadability, In vitro drug release was evaluated Drug content ranging from to 82.6 % to 91.24% entrapment efficiency values are ranged from 91.25% to 94.02% and in -vitro drug release studies are also studied. The In-vitro drug release study of Ofloxacin was carried out by using In-vitro diffusion apparatus.100ml of using tear fluid was taken in a beaker. The solution was stirred with 100rpm by maintaining the temperature of 37˚c ± 5˚c. The drug release data were explored for this type of release mechanism followed. The best fit with the highest determination R2 coefficients was shown by both the models (zero and peppas) followed by Higuchi model which indicate the drug release via diffusion mechanism. However as indicated by the values of R both of the models (zero and peppas) followed by Higuchi model were found to be efficient in describing the release of Ofloxacin.

Formulation and In Vivo Evaluation of Mucoadhesive Micro-spheres of Rebamipide, a Mucoprotective Drug for GIT Disorders

2018 ◽  
Vol 11 (3) ◽  
pp. 4089-4097
Author(s):  
Bhikshapathi D. V. R. N. ◽  
Kanteepan P
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
In Vivo Studies ◽  
Amino Acid Derivative ◽  
Release Mechanism ◽  
In Vivo Evaluation ◽  
In Vitro Drug Release ◽  
Percentage Yield

Rebamipide, an amino acid derivative of 2-(1H)-quinolinone, is used for mucosal protection, healing of gastroduodenal ulcers, and treatment of gastritis. The current research study aimed to develop novel gastro-retentive mucoadhesive microspheres of rebamipide using ionotropic gelation technique. Studies of micromeritic properties confirmed that microspheres were free flowing with good packability. The in vitro drug release showed the sustained release of rebamipide up to 99.23 ± 0.13% within 12 h whereas marketed product displayed the drug release of 95.15 ± 0.23% within 1 h. The release mechanism from microspheres followed the zero-order and Korsmeyer-Peppas (R2 = 0.915, 0.969), respectively. The optimized M12 formulation displayed optimum features, such as entrapment efficiency 97%, particle size 61.94 ± 0.11 µm, percentage yield 98%, swelling index 95% and mucoadhesiveness was 97%. FTIR studies revealed no major incompatibility between drug and excipients. SEM confirmed the particles were of spherical in shape. Optimized formulation (M12) were stable at 40°C ± 2°C/75% RH ± 5% RH for 6 months. In vivo studies were performed and kinetic parameters like Cmax, Tmax, AUC0-t, AUC0-∞, t1/2, and Kel  were calculated. The marketed product Cmax (3.15 ± 0.05 ng/mL) was higher than optimized formulation (2.58 ± 0.03 ng/mL). The optimized formulation AUC0-t (15.25 ± 1.14 ng.hr/mL), AUC0-∞ (19.42 ± 1.24 ng.hr/mL) was significantly higher than that of marketed product AUC0-t (10.21 ± 1.26 ng.hr/mL) and AUC0-∞ (13.15 ± 0.05 ng.hr/mL). These results indicate an optimized formulation bioavailability of 2.5-fold greater than marketed product.  

Preparation and Characterization of Mucoadhesive Microcapsules of Gliclazide with Natural Gums

1970 ◽  
Vol 4 (1) ◽  
pp. 38-48 ◽  
Author(s):  
Santhosh Kumar Mankala ◽  
Nishanth Kumar Nagamalli ◽  
Ramakrishna Raprla ◽  
Rajyalaxmi Kommula
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Guar Gum ◽  
Release Kinetics ◽  
Insulin Dependent Diabetes Mellitus ◽  
Dependent Diabetes Mellitus ◽  
Release Mechanism ◽  
Ionic Gelation ◽  
Release Formulation

Gliclazide is an oral hypoglycemic agent used in management of non-insulin dependent diabetes mellitus. Among people who are suffering from long term disorders, the major were categorized under diabetes so, a dosage form is needed to provide continuous therapy with high margin of safety & such dosage form can be achieved by microencapsulation. Gliclazide microspheres with sodium alginate (coat material, gum kondagogu, gum guar and xanthan gum (mucoadhesive agents) were prepared by orifice-ionic gelation and emulsification ionic gelation techniques varying concentrations (1:0.25, 1:0.5, 1:0.75 and 1:1). Formulations were then evaluated for surface morphology, particle shape, Carr’s index, microencapsulation efficiency, drug release, mucoadhesion studies. Compatibility studies were performed by FTIR, DSC, and XRD techniques and no interactions were found between drug and excepients used. The microspheres were found spherical and free flowing with emulsion ionic gelation technique with a size range 400-600μm. % drug content and encapsulation efficiency found in the range of 55%-68% and, 86.23%-94.46% respectively. All microspheres showed good mucoadhesive property in in-vitro wash of test. In vitro drug release studies showed that the guar gum has more potentiality to retard the drug release compared to other gums and concentrations. Drug release from the microspheres was found slow following zero order release kinetics with non-fickian release mechanism stating release depended on the coat: core ratio and the method employed. The concentration of 1:1 of SA: GG (EMG 4) found suitable for preparing the controlled release formulation of gliclazide stating emulsification gelation technique is the best among followed.   Key words: Gliclazide; Natural gums; orifice ionic gelation technique; emulsification ionic gelation technique DOI: http://dx.doi.org/10.3329/sjps.v4i1.8865 SJPS 2011; 4(1): 38-48

scholarly journals Design, Development and Evaluation Of Anti-Hypertensive Drug Solid Lipid Nano Particles

2021 ◽  
Vol 11 (4) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Wide Range

Recently, solid lipid Nano-particles have received much attention by the researchers owing to its biodegradability, biocompatibility and the ability to deliver a wide range of drugs. The aim of the present study was to design Diltiazem solid lipid Nano-particles and to evaluate them. Diltiazem solid lipid Nano-particles were prepared by hot homogenization technique using different lipids (Tristearin, GMS and Comprital), soy lecithin as stabilizers and tween 80, Poloxamer as surfactants. The Nano-particles were evaluated for particle size & PDI, zeta potential, entrapment efficiency and in vitro drug release. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations were good within the range of 0.189 to 0.427. The zeta potential ranged from -10.5 to -29.6 Mv, Entrapment efficiency of all formulations were observed was in the range of 78.68 to 95.23 %. The cumulative percentage release of Diltiazem from different Diltiazem Nano-particles varied from 53.36 to 88.74% depending upon the drug lipid ratio and the type of lipid used. The average percentage of drug released from different SLNs after 24 hours showed in the following order: F9 (53.35%) < F6 (56.75%) < F4 (61.74%) < F7 (63.8%) < F5(67.77%) < F8(69.04%) < F3(75.31%) < F1(79.36%) <F2 (88.74%) respectively. The release kinetic studies showed that the release was first order diffusion controlled and the n values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Quasi-Fickian type (n-value of 0.47). Keywords: Diltiazem, solid lipid Nano-particles, FTIR, in vitro drug release.

Etoposide-Loaded Microparticles Prepared with Poly (Hydroxybutyrate-Co-Hydroxyvalerate) and Poly(-Caprolactone) Blends: Formulation, Characterization and in vitro Drug Release

1970 ◽  
Vol 1 (3) ◽  
pp. 251-256
Author(s):  
Patel J. K ◽  
Tank H. M
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Release Mechanism ◽  
Evaporation Process ◽  
In Vitro Drug Release ◽  
Drug Release Mechanism ◽  
Drug Entrapment Efficiency ◽  
Solvent Evaporation Process ◽  
Poly Caprolactone

The purpose of this research was to formulate and systematically evaluate etoposide-loaded microparticles. Etoposide microparticles containing poly(hydroxybutyrate-co-hydroxyvalerate) and poly(-caprolactone) were prepared by an emulsion/solvent evaporation process. Microparticles were discrete, spherical and free flowing. The microparticles showed high % of yeild and drug entrapment efficiency. Etoposide-loaded microparticles demonstrated drug sustained releases (up to 200 hours). The drug release mechanism was dependent on the presence of PCL in the microparticles. The release of etoposide caused an increase in the surface area of the microparticles. A Fickian release was determined for the microparticles prepared exclusively with P(HBHV), while non-Fickian release behaviors were found for the P(HBHV)/PCL microparticles.

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 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 FORMULATION AND DEVELOPMENT OF PRONIOSOMAL GEL FOR TOPICAL DELIVERY OF AMPHOTERICIN B

2022 ◽  
pp. 37-49
Author(s):  
REESHA PARVEZ BAIG ◽  
MOHAMMAD WAIS
Keyword(s):  
Drug Release ◽  
Amphotericin B ◽  
Patient Compliance ◽  
Entrapment Efficiency ◽  
Topical Delivery ◽  
Ionic Surfactant ◽  
Prolonged Release ◽  
In Vitro Drug Release ◽  
Drug Content

Objective: The present research work of Amphotericin B Proniosomal gel focuses on improving patient compliance by reducing the side effects of conventional intravenous injections and minimizing the problem of physical stability and to localize drug at site of action. Methods: Proniosomal gels are prepared by coacervation phase separation technique using different concentration of non-ionic surfactants (Span and Tween) for uniform vesicle formation, lecithin as permeation enhancer/membrane stabilizer and cholesterol as a vesicle cement providing prolonged release. Prepared gels were evaluated for their viscosity, pH, spreadability, entrapment efficiency, drug content uniformity, extrudability, in vitro drug release, permeability and stability studies. Results: Among the nine formulations, F2 (containing 10 mg drug, 250 mg Span 60, 50 mg Soya lecithin) was found to be promising. Fourier Transform infra-red (FT-IR) spectra studies represented no interaction and physicochemical characteristics were found within the limits. The percentages of drug content and entrapment efficiency were determined to be 95.16%±0.40 and 94.20%±0.20, respectively. In vitro drug release was about 95.72%±0.30. Conclusion: Proniosomal gel could constitute a promising approach for topical delivery of Amphotericin B by encapsulating it in non-ionic surfactant to provide patient compliance with cutaneous fungal infection, which was found to be safe, tolerable and efficacious.

scholarly journals Formulation and In-Vitro Evaluation of Niosomal drug Delivery in Cancer Chemotherapy

2017 ◽  
Vol 5 (04) ◽  
pp. 29-33
Author(s):  
Naresh Kalra ◽  
G. Jeyabalan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
The Body ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Ethanol Injection

Drug delivery systems are defined as formulations aim for transportation of a drug to the desired area of action within the body. The aim of the study was to investigate the feasibility of using Niosomes as a drug delivery system for Cisplatin By entrapment of drug in Niosomes, dose also could be reduced. Niosomes were prepared by Ethanol injection method using cholesterol and Surfactant. Particle size, zeta potential, entrapment efficiency and in vitro drug release studies were performed. The targeted niosome delivery system is composed of drug, surfactant and cholesterol. With regard to the influence of formulation variables on the percent drug loading (PDL), different compositions with varying ratios of surfactant and cholesterol were studied. In –Vitro drug release mechanism was studied for 24 hours.

Design and In vivo Evaluation of Palonosetron HCl Mouth Dissolving Films in the Management of Chemotherapy-Induced Vomiting

2017 ◽  
Vol 10 (6) ◽  
pp. 3929-3936
Author(s):  
Y. Srinivasa Rao ◽  
K. Adinarayana Reddy
Keyword(s):  
Drug Release ◽  
Patient Compliance ◽  
Onset Of Action ◽  
In Vivo Evaluation ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Surface Ph ◽  
Drug Content

Fast dissolving oral delivery systems are solid dosage forms, which disintegrate or dissolve within 1 minute in the mouth without drinking water or chewing. Mouth dissolving film (MDF) is a better alternate to oral disintegrating tablets due to its novelty, ease of use and the consequent patient compliance. The purpose of this work was to develop mouth dissolving oral films of palonosetron HCl, an antiemetic drug especially used in the prevention and treatment of chemotherapy-induced nausea and vomiting. In the present work, the films were prepared by using solvent casting method with various polymers HPMC E3, E5 & E15 as a film base synthetic polymer, propylene glycol as a plasticizer and maltodextrin and other polymers. Films were found to be satisfactory when evaluated for thickness, in vitro drug release, folding endurance, drug content and disintegration time. The surface pH of all the films was found to be neutral. The in vitro drug release of optimized formulation F29 was found to be 99.55 ± 6.3 7% in 7 min. The optimized formulation F29 also showed satisfactory surface pH, drug content (99.38 ± 0.08 %), disintegration time of 8 seconds and good stability. FTIR data revealed that no interaction takes place between the drug and polymers used in the optimized formulation. In vitro and in vivo evaluation of the films confirmed their potential as an innovative dosage form to improve delivery and quick onset of action of Palonosetron Hydrochloride. Therefore, the mouth dissolving film of palonosetron is potentially useful for the treatment of emesis disease where quick onset of action is desired, also improved patient compliance.

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