Design and Pharmaceutical Evaluation of a Nano-Enabled Crosslinked Multipolymeric Scaffold for Prolonged Intracranial Release of Zidovudine

Purpose. Nanomedicine explores and allows for the development of drug delivery devices with superior drug uptake, controlled release and fewer drug side-effects. This study explored the use of nanosystems to formulate an implantable drug delivery device capable of sustained zidovudine release over a prolonged period. Methods. Pectin and alginate nanoparticles were prepared by applying a salting out and controlled gelification approach, respectively. The nanoparticles were characterized by attenuated total reflectance-fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and dynamic light scattering (DLS) and were further evaluated for zidovudine (AZT) entrapment efficiency. Multipolymeric scaffolds were prepared by crosslinking carboxymethyl cellulose, polyethylene oxide and epsilon caprolactone for entrapment of zidovudine-loaded alginate nanoparticles to impart enhanced controlled release of zidovudine over the time period. Swelling and textural analysis were conducted on the scaffolds. Prepared scaffolds were treated with hydrochloric acid (HCl) to reduce the swelling of matrix in the hydrated environment thereby further controlling the drug release. Drug release studies in phosphate buffered saline (pH 7.4, 37°C) were undertaken on both zidovudine-loaded nanoparticles and native scaffolds containing alginate nanoparticles. Results. A higher AZT entrapment efficiency was observed in alginate nanoparticles. Biphasic release was observed with both nanoparticle formulations, exhibiting an initial burst release of drug within hours of exposure to PBS, followed by a constant release rate of AZT over the remaining 30 days of nanoparticle analysis. Exposure of the scaffolds to HCl served to reduce the drug release rate from the entrapped alginate nanoparticles and extended the AZT release up to 30 days. Conclusions. The crosslinked multipolymeric scaffold loaded with alginate nanoparticles and treated with 1% HCl showed the potential for prolonged delivery of zidovudine over a period of 30 days and therefore may be a potential candidate for use as an implantable device in treating Aids Dementia Complex. This article is open to POST-PUBLICATION REVIEW. Registered readers (see “For Readers”) may comment by clicking on ABSTRACT on the issue’s contents page.

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Combine Drug Delivery of Thymoquinone-Doxorubicin by Cockle Shellderived pH-sensitive Aragonite CaCO3 Nanoparticles

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681209666190508122540 ◽

2020 ◽

Vol 10 (4) ◽

pp. 518-533 ◽

Cited By ~ 2

Author(s):

Kehinde M. Ibiyeye ◽

Abu B.Z. Zuki ◽

Norshariza Nurdin ◽

Mokrish Ajat

Keyword(s):

Electron Microscopy ◽

Drug Delivery ◽

Calcium Carbonate ◽

Drug Release ◽

Release Kinetics ◽

Drug Loading ◽

Ph Sensitive ◽

Multiple Drug ◽

Burst Release ◽

Cockle Shell

Background: Cockleshell-derived aragonite calcium carbonate nanoparticles were prepared by the top-down approach for combine delivery of two types of drugs. Objective: The aim of this study was to synthesize and characterize thymoquinone-doxorubicin loaded cockle shell-derived aragonite calcium carbonate nanoparticle. Aragonite calcium carbonate nanoparticles encapsulating thymoquinone and doxorubicin alone were also prepared. Methods: The blank and drug-loaded nanoparticles were characterized by field emission scanning electron microscopy, transmission electron microscopy, Zeta potential, Fourier transformed infrared and X-ray diffraction. Drug delivery properties, in vitro drug release study at pH 7.4, 6 and 4.8, and effect of blank nanoparticles on MCF10A, 3T3, MDA MB231 cells were also analyzed. Results: The blank and drug-loaded nanoparticles were pleomorphic and their sizes varying from 53.65 ± 10.29 nm to 60.49 ± 11.36 nm with an overall negative charge. The entrapment efficiency of thymoquinone and doxorubicin were 41.6 and 95.8, respectively. The FTIR showed little alteration after loading thymoquinone and doxorubicin while XRD patterns revealed no changes in the crystallizations of nanoparticles after drug loading. The drug release kinetics of doxorubicin and thymoquinone from the nanoparticles showed a continuous and gradual release after an initial burst release was observed. At pH 4.8, about 100% of drug release was noticed, 70% at pH 6 while only 50% at pH 7.4. The cell viability was 80% at a concentration of 1000 ug/ml of blank nanoparticle. Conclusion: The cockle shell-derived pH sensitive aragonite calcium carbonate nanoparticle provides an effective and simple means of multiple drug delivery and function as a platform for pH controlled release of loaded therapeutic agents.

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Ciprofloxacin intercalated in fluorohectorite clay: identical pure drug activity and toxicity with higher adsorption and controlled release rate

RSC Advances ◽

10.1039/c7ra01384a ◽

2017 ◽

Vol 7 (43) ◽

pp. 26537-26545 ◽

Cited By ~ 16

Author(s):

E. C. dos Santos ◽

Z. Rozynek ◽

E. L. Hansen ◽

R. Hartmann-Petersen ◽

R. N. Klitgaard ◽

...

Keyword(s):

Drug Delivery ◽

Controlled Release ◽

Drug Release ◽

Adsorption Capacity ◽

Release Rate ◽

Controlled Drug Release ◽

Drug Effectiveness ◽

Pure Drug ◽

Synthetic Clay ◽

Very High

We present the use of the synthetic clay fluorohectorite (Fh) as a drug delivery system of the antibiotic ciprofloxacin. The adsorption capacity is very high, and Fh promotes controlled drug release without changing drug effectiveness and toxicity.

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Water Soluble Silicon Quantum Dots Grafted with Amoxicillin as a Drug Delivery System

Journal of Nanoscience and Nanotechnology ◽

10.1166/jnn.2020.17845 ◽

2020 ◽

Vol 20 (8) ◽

pp. 4624-4628 ◽

Cited By ~ 1

Author(s):

Dowoo Ki ◽

Honglae Sohn

Keyword(s):

Drug Delivery ◽

Quantum Dots ◽

Controlled Release ◽

Ultra Violet ◽

Water Soluble ◽

Burst Release ◽

Potential Candidate ◽

Silicon Quantum Dots ◽

Hydrolysis Of ◽

Soluble Silicon

Water soluble silicon quantum dots (Si QDs) are prepared and used for the measurement of the efficiency for the controlled release drug delivery. Amoxicillin, antibiotics, is covalently grafted with Si QDs through a surface derivatization reaction. Si QDs are embedded in hydrogel polymer. The release of amoxicillin has been measured by using Ultra violet-visible (UV-vis) absorption spectrometer. Amoxicillin-embedded hydrogels exhibit a burst release for 1 h, however covalently loaded Amoxi-Si QDs hydrogel composite exhibited very slow release. Absorption analysis reveals that the Si QDs exhibits a great potential candidate for controlled release of drug. The controlled drugrelease profiles depend on the hydrolysis of amoxicillin from the surface of Si QDs.

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Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v6i1.8883 ◽

2016 ◽

Vol 6 (1) ◽

Author(s):

Anamika Saxena Saxena ◽

Santosh Kitawat ◽

Kalpesh Gaur ◽

Virendra Singh

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery Systems ◽

Entrapment Efficiency ◽

Repeated Administration ◽

Alginate Beads ◽

Delivery Systems ◽

Sem Analysis ◽

Formulation Development

The main goal of any drug delivery system is to achieve desired concentration of the drug in blood or tissue, which is therapeutically effective and nontoxic for a prolonged period. Various attempts have been made to develop gastroretentive delivery systems such as high density system, swelling, floating system. The recent developments of FDDS including the physiological and formulation variables affecting gastric retention, approaches to design single-unit and multiple-unit floating systems, and their classification and formulation aspects are covered in detail. Gastric emptying is a complex process and makes in vivo performance of the drug delivery systems uncertain. In order to avoid this variability, efforts have been made to increase the retention time of the drug-delivery systems for more than 12 hours. The floating or hydrodynamically controlled drug delivery systems are useful in such application. Background of the research: Diltiazem HCL (DTZ), has short biological half life of 3-4 h, requires rather high frequency of administration. Due to repeated administration there may be chances of patient incompliance and toxicity problems. Objective: The objective of study was to develop sustained release alginate beads of DTZ for reduction in dosing frequency, high bioavailability and better patient compliance. Methodology: Five formulations prepared by using different drug to polymer ratios, were evaluated for relevant parameters and compared. Alginate beads were prepared by ionotropic external gelation technique using CaCl2 as cross linking agent. Prepared beads were evaluated for % yield, entrapment efficiency, swelling index in 0.1N HCL, drug release study and SEM analysis. In order to improve %EE and drug release, LMP and sunflower oil were used as copolymers along with sodium alginate.

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Formulation Development and Characterization of controlled release core in cup matrix tablets of venlafaxine HCl

Current Drug Therapy ◽

10.2174/1574885515666200331104440 ◽

2020 ◽

Vol 15 ◽

Author(s):

Balaji Maddiboyina ◽

Vikas Jhawat ◽

Gandhi Sivaraman ◽

Om Prakash Sunnapu ◽

Ramya Krishna Nakkala ◽

...

Keyword(s):

Controlled Release ◽

Drug Release ◽

Release Rate ◽

Zero Order ◽

Water Soluble ◽

Matrix Tablets ◽

Drug Dissolution ◽

Crystalline Cellulose ◽

Hydrophobic Polymers

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

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Chitosan/Silver Nanoparticle/Graphene Oxide Nanocomposites with Multi-Drug Release, Antimicrobial, and Photothermal Conversion Functions

Materials ◽

10.3390/ma14092351 ◽

2021 ◽

Vol 14 (9) ◽

pp. 2351

Author(s):

Zheng Su ◽

Daye Sun ◽

Li Zhang ◽

Miaomiao He ◽

Yulin Jiang ◽

...

Keyword(s):

Silver Nanoparticles ◽

Graphene Oxide ◽

Drug Release ◽

Release Rate ◽

Composite System ◽

Methyl Blue ◽

Burst Release ◽

Fluorescein Sodium ◽

Photothermal Conversion ◽

Dual Drug

In this work, we designed and fabricated a multifunctional nanocomposite system that consists of chitosan, raspberry-like silver nanoparticles, and graphene oxide. The room temperature atmospheric pressure microplasma (RT-APM) process provides a rapid, facile, and environmentally-friendly method for introducing silver nanoparticles into the composite system. Our composite can achieve a pH controlled single and/or dual drug release. Under pH 7.4 for methyl blue loaded on chitosan, the drug release profile features a burst release during the first 10 h, followed by a more stabilized release of 70–80% after 40–50 h. For fluorescein sodium loaded on graphene oxide, the drug release only reached 45% towards the end of 240 h. When the composite acted as a dual drug release system, the interaction of fluorescein sodium and methyl blue slowed down the methyl blue release rate. Under pH 4, both single and dual drug systems showed a much higher release rate. In addition, our composite system demonstrated strong antibacterial abilities against E. coli and S. aureus, as well as an excellent photothermal conversion effect under irradiation of near infrared lasers. The photothermal conversion efficiency can be controlled by the laser power. These unique functionalities of our nanocomposite point to its potential application in multiple areas, such as multimodal therapeutics in healthcare, water treatment, and anti-microbials, among others.

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Microorganism-based monodisperse microcapsules: encapsulation of the fungicide tebuconazole and its controlled release properties

RSC Advances ◽

10.1039/c5ra01629k ◽

2015 ◽

Vol 5 (32) ◽

pp. 25164-25170 ◽

Cited By ~ 6

Author(s):

Bo Zhang ◽

Teng Zhang ◽

Quanxi Wang ◽

Tianrui Ren

Keyword(s):

Controlled Release ◽

Powdery Mildew ◽

Drug Release ◽

Release Rate ◽

Drug Release Rate ◽

Burst Effect ◽

Initial Burst ◽

Release System ◽

Controlled Release System ◽

Monodisperse Microcapsules

A controlled release system was prepared, it based on UF modified PCC cells in which TEB are loaded into cells. It can control the drug release rate, depress the initial “burst effect”, and was efficacious in controlling wheat powdery mildew.

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Formulation and Evaluation of Luliconazole Microsponges Loaded Gel for Topical Delivery

Research Journal of Pharmacy and Technology ◽

10.52711/0974-360x.2021.01004 ◽

2021 ◽

pp. 5775-5780

Author(s):

Farhana Sultan ◽

Himansu Chopra ◽

Gyanendra Kumar Sharma

Keyword(s):

Controlled Release ◽

Drug Release ◽

Ethyl Cellulose ◽

Entrapment Efficiency ◽

Topical Delivery ◽

Production Yield ◽

In Vitro Drug Release ◽

Eudragit Rs ◽

Diffusion Studies

Microsponge containing Luliconazole (LCZ) with different proportion of drug:polymer (Ethyl cellulose and Eudragit RS 100) were obtained efficiently using Quasi-emulsion solvent diffusion method. Luliconazole is an anti-fungal drug used for the topical delivery. The purpose of the microsponge formulation is to control the release of LCZ drug to the skin through Microsponge Delivery System (MDS) known to be the novel technique which overcome the maximum concentration of active ingredient, frequency doses, and skin irritation. The prepared microsponges were examined using drug content, % production yield, % entrapment efficiency and in-vitro drug release. The formulation were subjected to in-vitro drug release studies for 6 hr in which it was concluded that Ethyl cellulose microsponges formulated by drug:polymer (1:1) and Eudragit RS 100 microsponges formulated by drug:polymer (1:3) showed maximum controlled release i.e., Increase in drug:polymer ratio (1:1 to 1:9) increased the production yield and entrapment efficiency of microsponges using Ethyl cellulose with no significant effect for Eudragit RS 100.Therefore, both formulation F1 and F2 was dispersed in carbopol gel preparation for controlled delivery of LCZ to the skin. Various physical parameters like pH, spreadability, viscosity and in-vitro drug diffusion studies were evaluated for the prepared gel formulations. Microsponge gel formulation i.e., FG1 showed better results for controlled release of 89.40% as compared to FG2 i.e., 92.18% over the period of 12 hrs which is performed in Franz Diffusion Cell. On basis of in-vitro diffusion studies for LCZ gel formulation, microsponges using Ethyl cellulose (FG1) was found to be best for its controlled release of LCZ for 12 hrs and followed zero order kinetics. Hence, formulated LCZ loaded gel have potential to treat fungal infections i.e., tinea pedis, tinea cruris and tinea corporis.

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FORMULATION AND EVALUATION OF PERINDOPRIL MICROENCAPSULES BY USING DIFFERENT POLYMER

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2017.v10i2.14899 ◽

2017 ◽

Vol 10 (2) ◽

pp. 153

Author(s):

Leena Jacob ◽

Abhilash Tv ◽

Shajan Abraham

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Release Rate ◽

Oral Drug Delivery ◽

Entrapment Efficiency ◽

Water Soluble ◽

Oral Drug ◽

Percentage Yield ◽

Drug Entrapment Efficiency

Objective: The study was carried out with an objective to achieve a potential sustained release oral drug delivery system of an antihypertensive drug, Perindopril which is a ACE inhibitor having half life of 2 hours. Perindopril is water soluble drug, so we can control or delay the release rate of drug by using release retarding polymers. This may also decrease the toxic side effects by preventing the high initial concentration in the blood.Method: Microcapsules were prepared by solvent evaporation technique using Eudragit L100 and Ethyl cellulose as a retarding agent to control the release rate and magnesium stearate as an inert dispersing carrier to decrease the interfacial tension between lipophilic and hydrophilic phase. Results: Prepared microcapsules were evaluated for the particle size, percentage yield, drug entrapment efficiency, flow property and in vitro drug release for 12 h. Results indicated that the percentage yield, mean particle size, drug entrapment efficiency and the micrometric properties of the microcapsules was influenced by various drug: polymer ratio. The release rate of microcapsules could be controlled as desired by adjusting the combination ratio of dispersing agents to retarding agents.Conclusion:Perindopril microcapsules can be successfully designed to develop sustained drug delivery, that reduces the dosing frequency and their by one can increase the patient compliance.

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FORMULATION AND EVALUATION OF SIMVASTATIN GASTRORETENTIVE DRUG DELIVERY SYSTEM

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2017v9i3.18763 ◽

2017 ◽

Vol 9 (3) ◽

pp. 55

Author(s):

Manjunath P. N. ◽

Satish C. S. ◽

Vasanti S. ◽

Preetham A. C. ◽

Naidu Ras

Keyword(s):

Drug Delivery ◽

Drug Release ◽

Drug Delivery System ◽

Delivery System ◽

Release Rate ◽

Drug Transport ◽

Hydroxypropyl Methylcellulose ◽

In Vitro Dissolution ◽

Dissolution Studies ◽

Viscosity Grade

Objective: The aim of this study was to formulate and evaluate gastro retentive drug delivery system (GRRDS) using an effervescent approach for simvastatin.Methods: Floating tablets were prepared using directly compressible polymers hydroxypropyl methylcellulose (HPMC) K100M, HPMC K4M and carboxymethylcellulose sodium (NaCMC). The prepared tablets were subjected to pre-formulation studies like Compressibility index, Hausner ratio and post compression parameters like buoyancy/floating test and In vitro dissolution study.Results: Drug-excipient compatibility studies performed with the help of FTIR instrument indicated that there were no interactions. The DSC thermogram of the formulations revealed that crystalline form of simvastatin existed in the formulation which was confirmed by X-ray powder diffraction. Dissolution studies indicated that there was a decrease in the drug release with an increase in the polymer viscosity. The tablets prepared with low-viscosity grade HPMC K4M exhibited short Buoyancy Lag Time and floated for a longer duration as compared with formulations containing high viscosity grade HPMC K100M. The ‘n’ value for dissolution studies for all the formulations was found to be in the range of 0.647 to 0.975 indicating non-Fickian or anomalous drug transport. Conclusion: The drug release rate and floating duration of tablets depended on the nature of the polymer and other added excipients. The release rate of the drug can be optimized by using different ratios of polymers and other excipients. The formulation F8 achieved the optimized batch and complied with all the properties of the tablets.

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