scholarly journals Diffusion of lidocaine hydrochloride from lipid microparticles

2009 ◽  
Vol 15 (1) ◽  
pp. 33-35 ◽  
Author(s):  
Rada Pjanovic ◽  
Radoslava Stojanovic ◽  
Milana Sajber ◽  
Jelena Veljkovic ◽  
Nevenka Boskovic-Vragolovic ◽  
...  
Keyword(s):  
Drug Release ◽  
Diffusion Rate ◽  
Drug Carriers ◽  
Lidocaine Hydrochloride ◽  
Diffusion Cell ◽  
Sustained Drug Release ◽  
Franz Diffusion Cell ◽  
Diffusion Rates ◽  
Hydrochloride Solution ◽  
Prolonged Drug Release

Lipid particles, as drug carriers, are of increasing research interest, because a sustained drug release and avoidance of side effects could be achieved by using them. Lidocaine hydrochloride is a very efficient local anesthetic, but it has a short effect. The objective was to prolong the effect of the drug by encapsulating lidocaine hydrochloride in phospholipids microparticles. Two different procedures were used for the preparation of phospholipids microparticles. In both cases, phosphatidylcholine and lysophosphatidylcholine were used for the preparation of microparticles in which 5 % w/w lidocaine hydrochloride solution was encapsulated. The standard Franz diffusion cell was used for the experimental diffusion rate determination. The obtained results show that diffusion rate from microparticles is significantly lower than from the lidocaine hydrochloride solution, which means that this kind of microparticles could be used for the prolonged drug release. There was no much difference in diffusion rates from microparticles obtained by different procedures. That indicates that only the composition of the particles membrane has an influence on the lidocaine hydrochloride release rate.

Ibuprofen sorption and release by modified natural zeolites as prospective drug carriers

Clay Minerals ◽  
2015 ◽  
Vol 50 (1) ◽  
pp. 11-22 ◽  
Author(s):  
D. Krajišnik ◽  
A. Daković ◽  
A. Malenović ◽  
M. Kragović ◽  
J. Milić
Keyword(s):  
Drug Release ◽  
Cetylpyridinium Chloride ◽  
Drug Carriers ◽  
Drug Formulation ◽  
Buffer Solution ◽  
Solution Ph ◽  
Before And After ◽  
Prolonged Drug Release

AbstractThe sorption of ibuprofen by modified natural zeolite composites at three concentration levels (10, 20 and 30 mmol/100 g) of cationic surfactants – benzalkonium chloride and cetylpyridinium chloride, in a buffer solution (pH 7.4), was studied. Characterization of the composites before and after ibuprofen sorption was performed by drug sorption and isotherm studies, zeta potential and Fourier Transform infrared spectroscopic analysis. The biopharmaceutical performance of cationic surfactant-modified zeolites as drug formulation excipients was evaluated by in vitro dissolution experiments from the composites with medium surfactant contents. The drug sorption was influenced by the surfactant type and amount used for the zeolite modification. Prolonged drug release over a period of 8 h (up to ~40%) was achieved with both groups of samples. The kinetic analysis showed that the drug release profiles were best fitted with the Higuchi and the Bhaskar models, indicating a combination of drug diffusion and ion exchange as the predominant release mechanisms.

scholarly journals Thermosensitive Interfacial Migration of 5-FU in the Microenvironment of Pluronic Block Copolymers

Polymers ◽  
2021 ◽  
Vol 13 (16) ◽  
pp. 2705
Author(s):  
Tz-Feng Lin ◽  
Shih-Hsuan Yeh
Keyword(s):  
Drug Release ◽  
Environmental Temperature ◽  
Pluronic F127 ◽  
Segment Length ◽  
High Concentration ◽  
Sustained Drug Release ◽  
Chemotherapy Drugs ◽  
Important Field ◽  
High Concentrations ◽  
Prolonged Drug Release

Chemotherapy is one of the most important ways to treat cancer. At present, chemotherapy medicines are mainly administered by intravenous injection or oral administration. However, systemic medical care requires the dosage of high concentrations of drugs to defeat the malignant tumor growth. In recent years, the use of polymer composites for local and sustained drug release has become an important field of research to minimize side effects due to high-concentration chemotherapy drugs. Here, 19F-{1H} heteronuclear Overhauser enhancement spectroscopy (HOESY) was used to study the micellular environment of the F-containing chemotherapeutic drug 5-FU in Pluronic F127, Pluronic L121, and F127/L121 binary blending composites. The distribution of 5-FU in micelles is related to the PEO and PPO segment length of Pluronic polymers and the environmental temperature. The drug release tests further confirm that if 5-FU medicines were loaded in the PPO segment inside the micelles, the purpose of the prolonged drug release carrier is achieved.

Formulation and Evaluation of Liposomes of Ketoconazole

2009 ◽  
Vol 1 (1) ◽  
Author(s):  
Rakesh Patel ◽  
Hardik Patel ◽  
Ashok Baria
Keyword(s):  
Thin Film ◽  
Drug Release ◽  
Physical Stability ◽  
Weight Ratio ◽  
Entrapment Efficiency ◽  
Diffusion Cell ◽  
In Vitro Drug Release ◽  
Franz Diffusion Cell ◽  
Soya Lecithin

Antifungal drug, Ketoconazole was encapsulated in liposomes for topical application. Ketoconazole liposomes were prepared by thin film hydration technique using soya lecithin, cholesterol and drug in different weight ratios. The prepared liposomes were characterized for size, shape, entrapment efficiency, in-vitro drug release (by franz diffusion cell) and physical stability. The studies demonstrated successful preparation of Ketoconazole liposomes and effect of soya lecithin: cholesterol weight ratio on entrapment efficiency and on drug release.

scholarly journals FORMULATION AND EVALUATION OF BESIFLOXACIN NON-ERODIBLE OCULAR INSERTS

2022 ◽  
pp. 148-155
Author(s):  
JAYASHRI A. PATIL ◽  
RAVINDRA B. PATIL
Keyword(s):  
Drug Release ◽  
Moisture Absorption ◽  
Diffusion Rate ◽  
Polyvinyl Pyrrolidone ◽  
Sustained Drug Release ◽  
Eudragit Rs ◽  
In Vitro Diffusion ◽  
Drug Reservoir ◽  
Ocular Insert

Objective: Ocular inserts offer many advantages over conventional dosage forms, like increased ocular residence, the possibility of releasing a drug at a slow and constant rate, accurate dosing, exclusion of preservatives, and increased shelf life. Besifloxacin is a very important drug for the treatment of infectious conjunctivitis. The present study was aimed to formulate and evaluate Besifloxacin Non-Erodible Ocular Insert using Pullulan and polyvinyl pyrrolidone as a drug reservoir, PEG 400 as a plasticizer, and Eudragit RS-100 as a rate-controlling membrane. Methods: Central composite design was employed to study the effect of independent variables, i.e., effects of Pullulan amount (X1) and PVP (X2) on the dependent variables, i.e., % moisture absorption and In vitro diffusion rate. After evaluation of all thirteen batches of ocular insert reservoir formulation, BSF2 and BSF4 were selected as a satisfactory formulation and was sandwiched between rate-controlling membrane, which was made up of Eudragit RS-100 (3 and 5%). Results: The drug content of all formulations was found to be in the range of 95.33 to 99.89 %. In vitro diffusion of Besifloxacin from reservoir formulations (BSF1 to BSF13) was found to be 62.44 to 70.62 %. In vitro diffusion rate of an ocular insert of Besifloxacin can offer benefits such as increasing residence time, prolonging drug release in the eye for 24 h. Eudragit RS-100, as a sustained drug release polymer, showed promising sustained released action. Conclusion: The study concluded that Besifloxacin non-erodible ocular inserts can be successfully developed using Pullulan and polyvinyl pyrrolidone, which will sustain the release of the drug also reduce the frequency of administration, and thereby may help to improve patient compliance.

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

2010 ◽  
Vol 2 (2) ◽  
Author(s):  
Neeraj Agrawal ◽  
M.J. Chandrasekar ◽  
U.V. Sara ◽  
Rohini A.
Keyword(s):  
Drug Release ◽  
Drug Level ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Alkaline Environment ◽  
Stomach Acid ◽  
Release Studies ◽  
Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Formulation and Evaluation of Chitosan-Polyaniline Nanocomposites for Controlled Release of Anticancer Drug Doxorubicin

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Dillip Kumar Behera ◽  
Kampal Mishra ◽  
Padmolochan Nayak
Keyword(s):  
Tensile Strength ◽  
Drug Release ◽  
Nanocomposite Films ◽  
Casting Method ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Clay Particles ◽  
Solution Casting Method ◽  
Nanoclay Content

In this present work, chitosan (CS) crosslink with polyaniline (PANI) with montmorilonite (MMT) called as (CSPANI/MMT) and CS crosslink with PANI without MMT called as (CS-PANI) were prepared by employing the solution casting method. Further the formation of nanocomposites CS-PANI/MMT and CS-PANI were investigated using XRD, FTIR, SEM and tensile strength. Water uptake and swelling ratio of the CS-PANI and CS-PANI/MMT were found to decrease with increase in concentration of clay. Mechanical properties of the CS-PANI and CS-PANI/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with increase in the nanoclay content. In vitro drug release study on CS-PANI and CS-PANI/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in the CS polymer matrix. Overall CSPANI/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PANI.

Stereocomplexation Assisted Assembly of Poly(γ-glutamic Acid)-graft-polylactide Nano-micelles and Their Efficacy as Anticancer Drug Carrier

2018 ◽  
Vol 18 (2) ◽  
pp. 302-311
Author(s):  
Shulin Dai ◽  
Yucheng Feng ◽  
Shuyi Li ◽  
Yuxiao Chen ◽  
Meiqing Liu ◽  
...  
Keyword(s):  
Glutamic Acid ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Cancer Drug ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Anti Cancer ◽  
Physical Interactions

Background: Micelles as drug carriers are characterized by their inherent instability due to the weak physical interactions that facilitate the self-assembly of amphiphilic block copolymers. As one of the strong physical interactions, the stereocomplexation between the equal molar of enantiomeric polylactides, i.e., the poly(L-lactide) (PLLA) and poly(D-lactide) (PDLA), may be harnessed to obtain micelles with enhanced stability and drug loading capacity and consequent sustained release. </P><P> Aims/Methods: In this paper, stereocomplexed micelles gama-PGA-g-PLA micelles) were fabricated from the stereocomplexation between poly(gama-glutamic acid)-graft-PLLA gama-PGA-g-PLA) and poly(gamaglutamic acid)-graft-PDLA gama-PGA-g-PLA). These stereocomplexed micelles exhibited a lower CMC than the corresponding enantiomeric micelles. Result: Furthermore, they showed higher drug loading content and drug loading efficiency in addition to more sustained drug release profile in vitro. In vivo imaging confirmed that the DiR-encapsulated stereocomplexed gama-PGA-g-PLA micelles can deliver anti-cancer drug to tumors with enhanced tissue penetration. Overall, gama-PGA-g-PLA micelles exhibited greater anti-cancer effects as compared with the free drug and the stereocomplexation may be a promising strategy for fabrication of anti-cancer drug carriers with significantly enhanced efficacy.

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

2020 ◽  
Vol 12 ◽  
Author(s):  
Sagar R. Pardeshi ◽  
Harshal A. Mistari ◽  
Rakhi S. Jain ◽  
Pankaj R. Pardeshi ◽  
Rahul L. Rajput ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Factorial Design ◽  
Water Solubility ◽  
Tween 80 ◽  
Drug Release Profile ◽  
Sustained Drug Release ◽  
Bacterial Conjunctivitis ◽  
Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

scholarly journals Development and In Vitro-In Vivo Evaluation of a Novel Sustained-Release Loxoprofen Pellet with Double Coating Layer

Pharmaceutics ◽  
2019 ◽  
Vol 11 (6) ◽  
pp. 260 ◽  
Author(s):  
Dongwei Wan ◽  
Min Zhao ◽  
Jingjing Zhang ◽  
Libiao Luan
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Diffusion Rate ◽  
Immediate Release ◽  
Pharmacokinetic Studies ◽  
Release Tablet

This study aimed to develop a novel sustained release pellet of loxoprofen sodium (LXP) by coating a dissolution-rate controlling sub-layer containing hydroxypropyl methyl cellulose (HPMC) and citric acid, and a second diffusion-rate controlling layer containing aqueous dispersion of ethyl cellulose (ADEC) on the surface of a LXP conventional pellet, and to compare its performance in vivo with an immediate release tablet (Loxinon®). A three-level, three-factor Box-Behnken design and the response surface model (RSM) were used to investigate and optimize the effects of the citric acid content in the sub-layer, the sub-layer coating level, and the outer ADEC coating level on the in vitro release profiles of LXP sustained release pellets. The pharmacokinetic studies of the optimal sustained release pellets were performed in fasted beagle dogs using an immediate release tablet as a reference. The results illustrated that both the citric acid (CA) and ADEC as the dissolution- and diffusion-rate controlling materials significantly decreased the drug release rate. The optimal formulation showed a pH-independent drug release in media at pH above 4.5 and a slightly slow release in acid medium. The pharmacokinetic studies revealed that a more stable and prolonged plasma drug concentration profile of the optimal pellets was achieved, with a relative bioavaibility of 87.16% compared with the conventional tablets. This article provided a novel concept of two-step control of the release rate of LXP, which showed a sustained release both in vitro and in vivo.

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