scholarly journals A Review of In Vitro Drug Release Test Methods for Nano-Sized Dosage Forms

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Susan D’Souza
Keyword(s):  
Drug Release ◽  
Real Time ◽  
Test Methods ◽  
Dosage Forms ◽  
Formulation Development ◽  
Advantages And Disadvantages ◽  
Set Up ◽  
Sample And Separate ◽  
Compendial Standards

This review summarizes the methods used to study real-time (37°C) drug release from nanoparticulate drug delivery systems and establish an IVIVC. Since no compendial standards exist, drug release is currently assessed using a variety of methods including sample and separate (SS), continuous flow (CF), dialysis membrane (DM) methods, and a combination thereof, as well as novel techniques like voltametry and turbidimetry. This review describes the principle of each method along with their advantages and disadvantages, including challenges with set-up and sampling. The SS method allows direct measurement of drug release with simple set-up requirements, but sampling is cumbersome. With the CF method, sampling is straightforward but the set-up is time consuming. Set-up as well as sampling is easier with the DM, but it may not be suitable for drugs that bind to the membrane. Novel methods offer the possibility of real-time drug release measurement but may be restricted to certain types of drugs. Of these methods, Level A IVIVCs have been obtained with dialysis, alone or in combination with the sample and separate technique. Future efforts should focus on developing mathematical models that describe drug release mechanisms as well as facilitate formulation development of nano-sized dosage forms.

scholarly journals Non-invasive, real-time reporting drug release in vitro and in vivo

2015 ◽  
Vol 51 (32) ◽  
pp. 6948-6951 ◽  
Author(s):  
Yanfeng Zhang ◽  
Qian Yin ◽  
Jonathan Yen ◽  
Joanne Li ◽  
Hanze Ying ◽  
...  
Keyword(s):  
Drug Release ◽  
Real Time ◽  
Near Infrared ◽  
Reporting System ◽  
Real Time Monitoring ◽  
Near Infrared Fluorescence ◽  
Non Invasive ◽  
Fluorescence Dye

Anin vitroandin vivodrug-reporting system is developed for real-time monitoring of drug release via the analysis of the concurrently released near-infrared fluorescence dye.

Formulation and Evaluation of Transdermal patch of Methimazole

2021 ◽  
pp. 4667-4672
Author(s):  
Nani Tadhi ◽  
Himansu Chopra ◽  
Gyanendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Transdermal Patch ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Drug Release Study ◽  
Percent Moisture ◽  
Release Study

Transdermal patch is a drug delivery device in which the drugs are incorporated and is design in such a way that it releases the drug in sustained and at predetermined rate to deliver the drug through the skin to the systemic circulation painlessly. The aim of this research study was to formulate a controlled and sustained release transdermal matrix type patch of Methimazole. The matrix patch was prepared by solvent casting method using a various polymer in different concentration, HPMC (hydrophilic), Eudragit RL100 and Ethyl cellulose (hydrophobic) polymer. Total 9 prototype formulation were prepared and it was subjected for various evaluation test; weight uniformity, Folding endurance, thickness, Drug content, percent moisture content, percent Moisture uptake and In-vitro drug release study using Franz diffusion cell. The in-vitro CDR% data was fit into kinetics model to see the release kinetics from the patches. The Formulation F5 was choosen as a best formulation according to in-vitro drug release study. The in-vitro release was found 81.12 % in 12 hours, it followed zero order kinetics. The nature of polymer and concentration ratio of polymers plays a crucial role for obtaining a good transdermal patch design; therefore optimisation is very important step to formulate a desired TDDS. Therefore the result of the study encourages a further study and is hopeful that the present study would contribute to the recent pharmaceutical research for formulation development.

Formulation development of folic acid conjugated PLGA nanoparticles for improved cytotoxicity of Caffeic acid phenethyl ester

2021 ◽  
Vol 09 ◽  
Author(s):  
Harshad S Kapare ◽  
Sathiyanarayanan L ◽  
Arulmozhi S ◽  
Kakasaheb Mahadik
Keyword(s):  
Folic Acid ◽  
Drug Release ◽  
Caffeic Acid ◽  
Caffeic Acid Phenethyl Ester ◽  
Therapeutic Effects ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Active Constituent

Background: Honey bee propolis is one of the natural product reported in various traditional systems of medicines including Ayurveda. Caffeic acid phenethyl ester (CAPE) is an active constituent of propolis which is well known for its anticancer potential. The therapeutic effects of CAPE are restricted owing to its less aqueous solubility and low bioavailability. Objective: In this study CAPE loaded folic acid conjugated nanoparticle system (CLFPN) was investigated to enhance solubility, achieve sustained drug release and improved cytotoxicity of CAPE. Methods: Formulation development, characterization and optimization were carried out by design of experiment approach. In vitro and in vivo cytotoxicity study was carried out for optimized formulations. Results: Developed nanoparticles showed particle size and encapsulation efficiency of 170 ± 2 - 195 ± 3 nm and 75.66 ± 1.52 - 78.80 ± 1.25 % respectively. Optimized formulation CLFPN showed sustained drug release over a period of 42 h. GI50 concentration was decreased by 46.09% for formulation as compared to CAPE in MCF-7 cells indicating targeting effect of CLFPN. An improved in vitro cytotoxic effect was reflected in in-vivo Daltons Ascites Lymphoma model by reducing tumor cells count. Conclusion: The desired nanoparticle characteristic with improved in vivo and in vitro cytotoxicity was shown by developed formulation. Thus it can be further investigated for biomedical applications.

scholarly journals Formulation Development and Evaluation of Mouth Dissolving Tablet of Aspirin by Using QbD Approach

2021 ◽  
Vol 20 (1) ◽  
pp. 19-29
Author(s):  
Nilima A Thombre ◽  
Pradeep S Ahire ◽  
Sanjay J Kshirsagar
Keyword(s):  
Drug Release ◽  
Quality By Design ◽  
Formulation Development ◽  
Compression Method ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Design Expert ◽  
32 Factorial Design ◽  
Mouth Dissolving Tablet

In the current investigations, mouth dissolving tablets (MDT) were developed by applying quality by design (QbD) approach. Direct compression method was applied for the preparation of MDT containing aspirin using 32 factorial design with quantity of drug, microcrystalline cellulose (MCC) and crosscarmellose sodium (CCS) as dependant variables. MCC and CCS were used as superdisintegrants. Sodium stearyl fumarate was used as lubricant. Developed MDT were evaluated for characteristics like hardness, friability, disintegration time (DT) and in vitro drug release . Design Expert 11.0 described adequately impact of selected variables (MCC and CCS) at various levels for response under study (DT and friability). The optimized batch showed disintegration time of 15-28 secs, friability within 1% and in vitro drug release of 75-98% after 30 mins, respectively. The present study of experimental design revealed that MCC and CCS are fruitful at low concentration to develop the optimized formulation. As per the results obtained from the experiments, it can be concluded that QbD is an effective and efficient approach for the development of quality into MDT with the application of QTPP, risk assessment and critical quality attributes (CQA). Dhaka Univ. J. Pharm. Sci. 20(1): 19-29, 2021 (June)

scholarly journals NIR-Responsive Lysosomotropic Phototrigger: ʽAIE + ESIPTʼ Active Naphthalene Based Single Component Photoresponsive Nanocarrier with Two-Photon Uncaging and Real-Time Monitoring Ability

2021 ◽  
Author(s):  
Biswajit Roy ◽  
Rakesh Mengji ◽  
Samrat Roy ◽  
Bipul Pal ◽  
Avijit Jana ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Real Time ◽  
Near Infrared ◽  
Single Component ◽  
Photon Absorption ◽  
Real Time Monitoring ◽  
Two Photon ◽  
Nir Light

In recent times, organelle-targeted drug delivery systems gained tremendous attention due to the site specific delivery of active drug molecules resulting in enhanced bioefficacy. In this context, the phototriggered drug delivery system (DDS) for releasing an active molecule is superior as it provides spatial and temporal control over the release. So far, near infrared (NIR) light responsive organelle targeted DDS has not yet been developed. Hence, we introduced a two-photon NIR-light responsive lysosome targeted ʽAIE + ESIPTʼ active single component DDS based on naphthalene chromophore. The Two-photon absorption cross-section of our DDS is 142 GM at 850 nm. The DDS was converted into pure organic nanoparticles for biological applications. Our nano-DDS is capable of selective targeting, AIE-luminogenic imaging, and drug release within the lysosome. In vitro studies using cancerous cell lines showed that our single component photoresponsive nanocarrier exhibited enhanced cytotoxicity and real-time monitoring ability of the drug release.

scholarly journals Formulation, Development and Evaluation of Ibuprofen Loaded Nano-transferosomal Gel for the Treatment of Psoriasis

2019 ◽  
pp. 1-8
Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  
Keyword(s):  
Drug Release ◽  
Zeta Potential ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Formulation Development ◽  
In Vitro Drug Release ◽  
Vesicle Size

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.

scholarly journals Formulation Development and Evaluation of Drug Release Kinetics from Colon-Targeted Ibuprofen Tablets Based on Eudragit RL 100-Chitosan Interpolyelectrolyte Complexes

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kenneth Chibuzor Ofokansi ◽  
Franklin Chimaobi Kenechukwu
Keyword(s):  
Drug Release ◽  
Targeted Delivery ◽  
Release Kinetics ◽  
Local Treatment ◽  
Wet Granulation ◽  
Formulation Development ◽  
Swelling Properties ◽  
Interpolyelectrolyte Complexes ◽  
Bowel Diseases

Colon-targeted drug delivery systems (CTDDSs) could be useful for local treatment of inflammatory bowel diseases (IBDs). In this study, various interpolyelectrolyte complexes (IPECs), formed between Eudragit RL100 (EL) and chitosan (CS), by nonstoichiometric method, and tablets based on the IPECs, prepared by wet granulation, were evaluated as potential oral CTDDSs for ibuprofen (IBF). Results obtained showed that the tablets conformed to compendial requirements for acceptance and that CS and EL formed IPECs that showed pH-dependent swelling properties and prolonged the in vitro release of IBF from the tablets in the following descending order: 3 : 2 > 2 : 3 > 1 : 1 ratios of CS and EL. An electrostatic interaction between the carbonyl (–CO–) group of EL and amino (–) group of CS of the tablets formulated with the IPECs was capable of preventing drug release in the stomach and small intestine and helped in delivering the drug to the colon. Kinetic analysis of drug release profiles showed that the systems predominantly released IBF in a zero-order manner. IPECs based on CS and EL could be exploited successfully for colon-targeted delivery of IBF in the treatment of IBDs.

scholarly journals Formulation development and characterization of fast disintegrating tablets of Nimesulide

2012 ◽  
Vol 4 (2) ◽  
pp. 25-28
Author(s):  
Manoj M Nitalikar ◽  
Dinesh M Sakarkar
Keyword(s):  
Drug Release ◽  
Critical Concentration ◽  
Formulation Development ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Sodium Starch Glycolate ◽  
Evaluation Parameters ◽  
Fast Disintegrating Tablets

An attempt was made to prepare fast dissolving tablets of anti-inflammatory drug Nimesulide preparing by direct compression method. The superdisintegrants Cross-carmellose and Sodium starch glycolate were used in different concentrations. Twelve formulations using those superdisintegrants at different concentration levels were prepared to access their efficiency and critical concentration level. Different evaluation parameters for tablet were studied. Tablets containing Cross-carmellose showed superior organoleptic properties and excellent in-vitro drug release as compared to other formulations. It was observed that on increasing the concentration of Cross-carmellose, the rate of disintegration was increased whereas on increasing the concentration of Sodium starch glycolate the rate of disintegration was decreased. The percentage drug release was observed as 96.32% when the concentration of Cross-carmellose was increased, whereas the same was not observed on increasing the concentration of Sodium starch glycolate. DOI: http://dx.doi.org/10.3329/sjps.v4i2.10436 S. J. Pharm. Sci. 4(2) 2011: 25-28

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