Polymeric nanoparticles containing diazepam: preparation, optimization, characterization, in-vitro drug release and release kinetic study

The objective of the present study was to achieve the successful encapsulation of a therapeutic agent to achieve antifouling functionality regarding biomedical applications. Considering nanotechnology, drug-loaded polycaprolactone (PCL)-based nanoparticles were prepared using a nano-precipitation technique by optimizing various process parameters. The resultant nano-formulations were investigated for in vitro drug release and antifouling applications. The prepared particles were characterized in terms of surface morphology and surface properties. Optimized blank and drug-loaded nanoparticles had an average size of 200 nm and 216 nm, respectively, with associated charges of −16.8 mV and −11.2 mV. Studies of the in vitro release of drug were carried out, which showed sustained release at two different pH, 5.5 and 7.4 Antifouling activity was observed against two bacterial strains, Gram-positive Staphylococcus aureus and Gram-negative Escherichia coli. The zone of inhibition of the optimized polymeric drug-loaded nanoparticle F-25 against both strains were compared with the pure drug. The gradual pH-responsive release of antibiotics from the biodegradable polymeric nanoparticles could significantly increase the efficiency and pharmacokinetics of the drug as compared to the pure drug. The acquired data significantly noted that the resultant nano-encapsulation of antifouling functionality could be a promising candidate for topical drug delivery systems and skin applications.

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FORMULATION AND IN VITRO–IN VIVO PHARMACOKINETIC EVALUATION OF CARDIOVASCULAR DRUG-LOADED PULSATILE DRUG DELIVERY SYSTEMS

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i6.42607 ◽

2021 ◽

pp. 144-151

Author(s):

KUMAR BABU PASUPULETI ◽

VENKATACHALAM A. ◽

BHASKAR REDDY KESAVAN

Keyword(s):

Drug Release ◽

Ethyl Cellulose ◽

Release Kinetic ◽

In Vitro Drug Release ◽

The Core ◽

Coated Tablet ◽

Tablet Formulations ◽

Core Tablet

Objective: This study is to formulate Nebivolol into a Pulsatile liquid, solid composite compression coated tablet, which will delay the release of the drug in early morning hypertension conditions. Methods: The liquid, solid composite tablet was formulated and compressed with the ethylcellulose coating polymer. The percent in vitro drug release of the liquid solid composite compressed tablet was tested. Based on disintegration time and wetting time, the LCS2, LCS3, LSC6, LCS7 and LCS12 formulations were found to be the optimized solid-liquid compacts fast-dissolving core tablet formulations, which may be excellent candidates for further coating with polymer to transfer into press coated pulsatile tablet formulations. Coating the core tablet with varying ethyl cellulose concentrations resulted in five different formulations of the pulsatile press-coated tablet (CT1, CT2, CT3, CT4, CT5). In vitro drug release, in vitro release, kinetic studies, in vivo pharmacokinetic and stability tests were all performed for the prepared pulsatile press coated tablet. Results: CT3 tablets are coated with ethyl cellulose polymer, which shows maximum controlled drug release from the core tablet i.e. 96.34±1.2% at 8th h. It shows there was an efficient delay in drug release form core tablet i.e. up to 3 h, followed by the maximum amount of drug release of 96.34±2.4 at 8h. Which shows the core drug will be more efficiently protected from the gastric acid environment 1.2 pH, duodenal environment 4.0 pH and release drug only in the small intestine. Conclusion: According to the findings, CT3 Pulsatile press-coated tablet increased the bioavailability of Nebivolol by 3.11 percent.

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FORMULATION AND EVALUATION OF NATEGLINIDE NANOSPONGES

INDIAN DRUGS ◽

10.53879/id.55.02.10717 ◽

2018 ◽

Vol 55 (02) ◽

pp. 27-35

Author(s):

A. A Bakliwal ◽

◽

D. S. Jat ◽

S. G. Talele ◽

A. G. Jadhav

Keyword(s):

Particle Size ◽

Drug Release ◽

Release Kinetics ◽

Synthesis Method ◽

Ultra Sound ◽

Size Analysis ◽

Release Kinetic ◽

In Vitro Drug Release ◽

Drug Content

The objective of the present study was to produce extended release nateglinide nanosponges for oral delivery. Preparation of nanosponges leads to solubility enhancement. Nateglinide is a BCS Class II drug, having low solubility. So, to increase the solubility of nateglinide it is formulated into nanosponges. Nanosponges using ethyl cellulose as a polymer and dichloromethane as a cross-linker were prepared successfully by ultra-sound assisted synthesis method. The effects of different drug: placebo ratios on the physical characteristics of the nanosponges as well as the drug content and in vitro drug release of the nanosponges were investigated. Particle size analysis and surface morphology of nanosponges were performed. The scanning and transmission electron microscopy of nanosponges showed that they were spongy in nature. The particle size was found to be in the range 46.37 - 97.23 nm out of which particle size of the optimized formulation was 51.79 nm and the drug content was found to 79.43 %. The optimized nanosponge formulations were selected for preparing nanosponge tablets for extended drug delivery by oral route. These tablets were prepared using xanthan gum and PVP K-30 and were evaluated by pre-compression and post-compression parameters. The nateglinide nanosponges tablet formulation were studied for different parameters using Design Expert Software. All formulations were evaluated for in vitro drug release analyzed according to various release kinetic models and it was found that it follows zero order release kinetics.

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FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLETS OF LEVOSULPIRIDE BY USING NATURAL POLYMER

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i5.17475 ◽

2017 ◽

Vol 10 (5) ◽

pp. 285

Author(s):

S Shanmugam

Keyword(s):

Drug Release ◽

Sustained Release ◽

Xanthan Gum ◽

Diffusion Mechanism ◽

Matrix Tablets ◽

In Vitro Dissolution ◽

Release Kinetic ◽

Natural Polymers ◽

In Vitro Drug Release

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism. Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies

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Development of Nasal Mucoadhesive Microspheres of Granisetron: A Potential Drug

Drug Research ◽

10.1055/a-1193-4781 ◽

2020 ◽

Vol 70 (08) ◽

pp. 367

Author(s):

Jaideo Pandey ◽

Ravi Shankar ◽

Manish Kumar ◽

Kuldeep Shukla ◽

Beena Kumari

Keyword(s):

Drug Release ◽

Residence Time ◽

Stability Study ◽

Nasal Delivery ◽

Release Kinetic ◽

In Vitro Drug Release ◽

Model Study ◽

Maximum Stability ◽

Pass Metabolism

Abstract Background Granisetron is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy and radiotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. Objectives In this research mucoadhesive microspheres were developed in order to carry out the absorption of drug through nasal mucosa with the aim to improve therapeutic efficacy, avoid hepatic first pass metabolism and increase residence time. Material and Methods Mucoadhesive microspheres of Granisetron using chitosan as polymer were prepared by emulsification cross-linking method to increase the residence time on the mucosa. The surface of prepared microspheres was characterized by SEM (Scanning electron microscopy) and evaluated for particle size, encapsulation efficiency, production yield, swelling ability, in-vitro mucoadhesion, in-vitro drug release and stability study. Result Among all the formulations F6 with drug/polymer ratio of 1:3 displayed the best result. On drug release kinetic model study, all the formulations follow Zero order. Stability studies revealed that the microspheres kept at 25±2°C and 60±5% RH showed the maximum stability. Conclusion After all the evaluation parameters and result obtained it can be said that these results confirmed the suitability of Granisetron mucoadhesive chitosan microspheres for nasal delivery system.

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Preparation, characterization and in vitro drug release studies of novel polymeric nanoparticles

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2006.05.065 ◽

2006 ◽

Vol 323 (1-2) ◽

pp. 146-152 ◽

Cited By ~ 25

Author(s):

Surendra Nimesh ◽

Romila Manchanda ◽

Rupesh Kumar ◽

Amit Saxena ◽

Preeti Chaudhary ◽

...

Keyword(s):

Drug Release ◽

Polymeric Nanoparticles ◽

In Vitro Drug Release ◽

Release Studies

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EMULSOMES FOR LIPOPHILIC ANTICANCER DRUG DELIVERY: DEVELOPMENT, OPTIMIZATION AND IN VITRO DRUG RELEASE KINETIC STUDY

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i2.40339 ◽

2021 ◽

pp. 114-121

Author(s):

S. DUBEY ◽

S. P. VYAS

Keyword(s):

Drug Release ◽

Release Kinetics ◽

Particle Diameter ◽

Release Profile ◽

Water Soluble ◽

Fickian Diffusion ◽

Release Kinetic ◽

In Vitro Drug Release ◽

Solid Lipid

Objective: The objective of the present study was to formulate and characterize paclitaxel (Ptx) loaded sterically stabilized emulsomes to provide non-toxic and biocompatible carriers with high Ptx loading efficiency. Methods: Plain (P-Es) and sterically stabilized emulsomes (SS-Es) were prepared by a modified solvent evaporation method using tristearin as solid lipid and optimized for lipid to (DSPC+CHOL+DSPE-PEG)/ tristearin ratio, lipid/lipid-PEG (DSPC+CHOL/DSPE-PEG) molar ratio, solid lipid concentration, phospholipid concentration, organic to aqueous phase volume and homogenization time based on their effect particle size and entrapment efficiency. Optimized emulsomes were characterized for morphological features, in vitro drug release kinetics and protection from plasma protein. Results: The emulsomes so formed were uniform in size with a mean particle diameter of 275±5.52 and 195±6.4 nm for P-Es and SS-Es respectively. All the formulations showed pH dependent drug release with a slow and sustained release profile. Slower drug release was observed from sterically stabilized emulsomes than the plain emulsomes. The drug release profile followed the Higuchi model with the Fickian diffusion pattern. The Pegylation of emulsomes significantly reduced the in vitro protein absorption. Conclusion: The sterically stabilized emulsome can serve as a novel non-toxic platform with longer circulatory time for the delivery of Paclitaxel and other poorly water-soluble drugs as well.

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An Innovative Approach for Development and Evaluation of Nanosized Lamotrigine Loaded Bionanoparticles Using Biopolymer from Fragaria × ananassa Fruit

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2020.13.4.4 ◽

2020 ◽

Vol 13 (4) ◽

pp. 4990-4999

Author(s):

Sushant Kumar ◽

Satheesh Madhav N V ◽

Anurag Verma ◽

Kamla Pathak

Keyword(s):

Particle Size ◽

Drug Release ◽

Kinetic Study ◽

In Vitro Release ◽

Release Kinetic ◽

Fruit Pulp ◽

Fragaria Ananassa ◽

Release Study ◽

Vitro Release

The purpose of this research was to isolate the smart biopolymer from the fruit pulp of Fragaria × ananassa (garden strawberry). We isolated natural fruit pulp to evaluate the potentiality of biopolymer in delivery of nanosized lamotrigine as an antiepileptic drug. Lamotrigine was nanosized by screening its nano-size particle by UV method. The nanosized lamotrigine was used for preparation of bionanoparticles (LF1-LF8) by sonication method. The isolated biopolymer was characterized for DSC, FTIR, NMR, Mass and Zeta particle size analysis. The obtained results confirm its polymeric nature in different analysis. The prepared bionanoparticles showed the release of lamotrigine in sustained manner over 36 hours. The release kinetic study was done by using the BIT-SOFT 1.12 software and T50% and T80%, r2 were calculated. All the formulation showed more than 99.78% drug release. The In-vitro release study of different formulations showed the % drug release from 90.92% to 99.78%. The different formulations were evaluated for the In-vitro release study and release kinetic was studied. The formulation LF5 was found to be the best formulation having T50% of 17 hours and T80% of 29 hours with r2 value of 0.9925. The best formulation LF5 showed up to 90.925% drug release over 36 hours. According to the release kinetic study, the best-fit model was found to be Koresmayer-Peppas and the mechanism of drug release was found to be anomalous transport. The results obtained from different evaluations like percentage entrapment efficiency, particle size, release study, kinetic studies and stability study revealed that isolated biopolymer has good potentiality to form bionanoparticles and it can be safely used as an alternative to synthetic and semisynthetic polymers for the preparation of lamotrigine loaded stable bionanoparticles

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Pharmaceutical Development and Evaluation of Reservoirtype Ciprofloxacin Ocular Insert

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.4.5 ◽

2015 ◽

Vol 8 (4) ◽

pp. 3024-3030

Author(s):

Jayesh K Jethva ◽

Chintan H Trivedi ◽

Sarita P Ratanpara ◽

Geeta R Bathwar ◽

Ramesh B Parmar

Keyword(s):

Drug Release ◽

Moisture Absorption ◽

Compartment Model ◽

Moisture Loss ◽

Physical Parameters ◽

Release Kinetic ◽

In Vitro Drug Release ◽

Percent Moisture ◽

Drug Reservoir

Ocular inserts of ciprofloxacin hydrochloride were prepared with the aim of achieving once a day administration. Drug reservoir was prepared using sodium CMC while rate controlling membrane was prepared using Eudragit RS100 and RL100. Ocular inserts were evaluated for their physicochemical parameters like thickness, weight uniformity, drug content, percent moisture loss, and percent moisture absorption. The in vitro drug release studies were carried out using Bi-chambered donor receiver compartment model. In vitro drug release kinetic data was treated according to Zero, First, and Higuchi kinetics to access the mechanism of drug release. At the end of 24th hr, in-vitro percentage drug release was obtained for the formulations RF1 was% 46.02 and for RF5 was 98.23%. The drug release from the formulation RF5 (Eudragit RS and RL 100 (1:1)) was 98.23 % at the end of 24th hour which was available as controlled and prolonged. In Kors Meyer Peppas, n value in optimized batch (RF5) was observed 1.399 which indicated super case II transport occurs. All physical parameters evaluated were satisfactory. So formulation RF5 was selected as the best formulation.

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