scholarly journals SALICYLIC ACID INCORPORATION IN Fe3O4-BSA NANOPARTICLES FOR DRUG RELEASE

Química Nova ◽  
2021 ◽  
Author(s):  
Renata Neves ◽  
Erika Bronze-Uhle ◽  
Pâmela Santos ◽  
Paulo Lisboa-Filho ◽  
Aroldo Magdalena
Keyword(s):  
Salicylic Acid ◽  
Controlled Release ◽  
Colloidal Stability ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Drug Loading ◽  
Release Mechanism ◽  
The Matrix ◽  
Collateral Effects ◽  
Average Size

The controlled release of Salicylic Acid (SA) influences the concentration and collateral effects of the drug. This release refers to the matrix in which the SA is incorporated. Among the matrices, Fe3O4 nanoparticles (NPs) stand out, for transporting drugs to specific sites. The functionalization of Fe3O4 by bovine serum albumin (BSA) can improve colloidal and chemical stability, in addition to increasing interactions with drugs. Thus, understanding the release kinetics of the AS incorporated in Fe3O4-BSA is essential to improve the controlled release. The study aimed the synthesis, characterization and release of the SA into the Fe3O4-BSA NPs. The results showed the functionalization of the Fe3O4-BSA NPs was effective and the average size was below 30 nm. The NPs showed colloidal stability above the pH of 7.5 which can be used as a drug carrier in blood plasma. Drug encapsulation into the NPs system was efficient (~91%) with about 30% of drug loading capability. The kinetic results showed the SA release mechanism was controlled by diffusion. The conclusion is that the incorporation of SA in Fe3O4-BSA NPs led to a release of SA in the first six hours, reaching equilibrium at 0.265 mg mL-1 and 1.83 mg.

Chitosan-based Polymer Matrix for Pharmaceutical Excipients and Drug Delivery

2019 ◽  
Vol 26 (14) ◽  
pp. 2502-2513 ◽  
Author(s):  
Md. Iqbal Hassan Khan ◽  
Xingye An ◽  
Lei Dai ◽  
Hailong Li ◽  
Avik Khan ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Drug Carrier ◽  
Drug Loading ◽  
Delivery Systems ◽  
Cancer Drug ◽  
Release Mechanism ◽  
Innovative Drug ◽  
Pharmaceutical Excipients ◽  
Weight Variation

The development of innovative drug delivery systems, versatile to different drug characteristics with better effectiveness and safety, has always been in high demand. Chitosan, an aminopolysaccharide, derived from natural chitin biomass, has received much attention as one of the emerging pharmaceutical excipients and drug delivery entities. Chitosan and its derivatives can be used for direct compression tablets, as disintegrant for controlled release or for improving dissolution. Chitosan has been reported for use in drug delivery system to produce drugs with enhanced muco-adhesiveness, permeation, absorption and bioavailability. Due to filmogenic and ionic properties of chitosan and its derivative(s), drug release mechanism using microsphere technology in hydrogel formulation is particularly relevant to pharmaceutical product development. This review highlights the suitability and future of chitosan in drug delivery with special attention to drug loading and release from chitosan based hydrogels. Extensive studies on the favorable non-toxicity, biocompatibility, biodegradability, solubility and molecular weight variation have made this polymer an attractive candidate for developing novel drug delivery systems including various advanced therapeutic applications such as gene delivery, DNA based drugs, organ specific drug carrier, cancer drug carrier, etc.

scholarly journals Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

2020 ◽  
Vol 6 (1) ◽  
Author(s):  
Chukwuebuka H. Ozoude ◽  
Chukwuemeka P. Azubuike ◽  
Modupe O. Ologunagba ◽  
Sejoro S. Tonuewa ◽  
Cecilia I. Igwilo
Keyword(s):  
Controlled Release ◽  
Sodium Alginate ◽  
Release Kinetics ◽  
Drug Carrier ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

scholarly journals Diatoms Green Nanotechnology for Biosilica-Based Drug Delivery Systems

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 242 ◽  
Author(s):  
Monica Terracciano ◽  
Luca De Stefano ◽  
Ilaria Rea
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Low Cost ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Drug Loading ◽  
Three Dimensional ◽  
Delivery Systems ◽  
Diatom Frustule ◽  
Artificial Environment

Diatom microalgae are the most outstanding natural source of porous silica. The diatom cell is enclosed in a three-dimensional (3-D) ordered nanopatterned silica cell wall, called frustule. The unique properties of the diatom frustule, including high specific surface area, thermal stability, biocompatibility, and tailorable surface chemistry, make diatoms really promising for biomedical applications. Moreover, they are easy to cultivate in an artificial environment and there is a large availability of diatom frustules as fossil material (diatomite) in several areas of the world. For all these reasons, diatoms are an intriguing alternative to synthetic materials for the development of low-cost drug delivery systems. This review article focuses on the possible use of diatom-derived silica as drug carrier systems. The functionalization strategies of diatom micro/nanoparticles for improving their biophysical properties, such as cellular internalization and drug loading/release kinetics, are described. In addition, the realization of hybrid diatom-based devices with advanced properties for theranostics and targeted or augmented drug delivery applications is also discussed.

scholarly journals Optimizing the Role of Polymer Blend in the Preparation of Acyclovir Controlled-Release Tablets: An Approach for Better Patient Compliance

2018 ◽  
Author(s):  
Barkat Khan ◽  
Faheem Haider ◽  
Kifayat Shah ◽  
Bushra Uzair ◽  
Kaijian Hou ◽  
...  
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Immediate Release ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solubility Study ◽  
Release Data

This study was carried out to formulate and evaluate controlled release (CR) matrix tablets of Acyclovir using combination of hydrophilic and hydrophobic polymers. Acyclovir is a guanine derivative and is its half-life is short hence administered five times a day using immediate release tablets. Six formulations (F1-F6) were developed using Ethocel and Carbopol in equal combinations at drug-polymer (D:P) ratio of 10:5, 10:6, 10:7, 10:8, 10:9 and 10:10. Solubility study was performed using six different solvents. The compatibility studies were carried out using FTIR and DSC. According to USP, Quality Control and dimensional tests (hardness, friability, disintegration and thickness) were executed. In-vitro drug release studies of Acyclovir was carried out in dissolution apparatus using using 0.1 N HCl medium at constant temperature of 37 ± 0.5 ºC. In order to analyze the drug release kinetics, five different mathematical models were applied to the release data. The results showed that there was no incompatibility between drug and polymers. Physical QC tests were found within limits of USP. The release was retarded upto 24 hrs and non-fickian in-vitro drug release mechanism was found. A formulation developed using blend of polymers, showed excellent retention and desired release profiles thus providing absolute control for 24 hrs.

Surface Engineered Porous Silicon-based Nanostructures for Cancer Therapy

2012 ◽  
Vol 1416 ◽  
Author(s):  
Adi Tzur-Balter ◽  
Naama Massad-Ivanir ◽  
Ester Segal
Keyword(s):  
Porous Silicon ◽  
Surface Chemistry ◽  
Electrochemical Etching ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Drug Loading ◽  
Nitrogen Adsorption ◽  
Cancer Drug ◽  
Cytotoxicity Studies

ABSTRACTIn this work, nanostructured porous silicon (PSi) hosts, synthesized by electrochemical etching of Si, are designed to carry and release the anti cancer drug, mitoxantrone dihydrochloride (MTX). We study the effect of surface chemistry of the Si scaffold on its properties as a drug carrier. The freshly-etched PSi is modified by surface alkylation using thermal hydrosilylation with 1-dodecene. Fourier-transform infrared spectroscopy and nitrogen adsorption-desorption measurements are employed to characterize the PSi carriers after chemical modification. Both, drug loading efficiency and release kinetics are found to be significantly affected by surface chemistry of the PSi. In vitro cytotoxicity studies on human breast carcinoma (MDA-MB-231) cells show that the MTX released from the PSi hosts maintains its cytotoxic functionality.

scholarly journals PREPARATION, CHARACTERISATION AND EVALUATION OF ROPINIROLE HYDROCHLORIDE LOADED CONTROLLED RELEASE MICROSPHERES USING SOLVENT EVAPORATION TECHNIQUE

2018 ◽  
Vol 10 (6) ◽  
pp. 57
Author(s):  
Koyel Kar ◽  
R. N. Pal ◽  
N. N. Bala
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
In Vitro Drug Release ◽  
Aqueous Solvent ◽  
Evaporation Technique ◽  
Ropinirole Hydrochloride

Objective: The major objective of the research work was to design, characterise and evaluate controlled release microspheres of ropinirole hydrochloride by using non-aqueous solvent evaporation technique to facilitate the delivery of the drug at a predetermined rate for a specific period of time.Methods: Ropinirole hydrochloride microspheres were prepared by using different low-density polymers such as eudragit RL 100, eudragit RS 100 and ethylcellulose either alone or in combination with the help of non-aqueous solvent evaporation technique. All the formulated microparticles were subjected to various evaluation parameters such as particle size analysis, micrometric properties, drug entrapment efficiency, percentage drug loading, percentage yield and in vitro drug release study. The compatibility of the drug and polymers was confirmed by physical compatibility study, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and x-ray diffraction study (XRD). The formation of the most optimized batch of the microsphere (F12) was confirmed by scanning electron microscopy (SEM), DSC, FTIR, and XRD. In vitro drug release study and in vitro drug release kinetics study of the formulated microspheres were also carried out.Results: Drug-polymer compatibility studies performed with the help of FTIR and DSC indicated that there were no interactions. Results revealed that non-aqueous solvent evaporation technique was a suitable technique for the preparation of microspheres as most of the formulations were discrete, free-flowing and spherical in shape with a good yield of 55.67% to 80.09%, percentage drug loading of 35.52% to 94.50% and percentage drug entrapment efficiency of 36.24% to 95.07%. Different drug-polymer ratios, as well as the combination of polymers, played a significant role in the variation of over-all characteristics of formulations. Based on the data of various evaluation parameters such as particle size analysis, percentage drug loading, percentage drug entrapment, percentage yield, rheological studies and in vitro drug release characteristics, formulation F12 was found to fulfil the criteria of ideal controlled release drug delivery system. F12 showed controlled release till the 14th hour (97.99%) and its in vitro release kinetics was best explained by zero-order kinetics and followed Korsemeyer-Pappas model (Non-Fickian mechanism). SEM of F12 revealed the formation of spherical structures. The FTIR study of F12 confirmed the stable nature of ropinirole in the drug-loaded microspheres. DSC and XRD patterns showed that ropinirole hydrochloride was dispersed at the molecular level in the polymer matrix.Conclusion: The controlled release microparticles were successfully prepared and from this study, it was concluded that the developed microspheres of ropinirole hydrochloride can be used for controlled drug release to improve the bioavailability and patient compliance and to maintain a constant drug level in the blood target tissue by releasing the drug in zero order pattern.

scholarly journals Resealed Erythrocytes as Drug Carriers and Its Therapeutic Applications

2017 ◽  
pp. 459-485
Author(s):  
Prabhakar Singh ◽  
Sudhakar Singh ◽  
Rajesh Kumar Kesharwani
Keyword(s):  
Drug Delivery ◽  
Blood Cells ◽  
Drug Delivery Systems ◽  
Release Kinetics ◽  
Drug Carrier ◽  
Drug Loading ◽  
Drug Carriers ◽  
Delivery Systems ◽  
The Body ◽  
Body Ideal

In this pharma innovative world, there are more than 30 drug delivery systems. Today's due to lacking the target specificity, the present scenario about drug delivery is emphasizing towards targeted drug delivery systems. Erythrocytes are the most common type of blood cells travel thousands of miles from wide to narrow pathways to deliver oxygen, drugs and nutrient during their lifetime. Red blood cells have strong and targeted potential carrier capabilities for varieties of drugs. Drug-loaded carrier erythrocytes or resealed erythrocytes are promising for various passive and active targeting. Resealed erythrocyte have advantage over several drug carrier models like biocompatibility, biodegradability without toxic products, inert intracellular environment, entrapping potential for a variety of chemicals, protection of the organism against toxic effects of the drug, able to circulate throughout the body, ideal zero-order drug-release kinetics, no undesired immune response against encapsulated drug etc. Resealed erythrocytes are rapidly taken up by macrophages of the Reticuloendothelial System (RES) of the liver, lung, and spleen of the body and hence drugs also. Resealed erythrocytes method of drugs delivery is secure and effective for drugs targeting specially for a longer period of time. This chapter will explain the different method of drug loading for resealed erythrocytes, their characterization, and applications in various therapies and associated health benefits.

scholarly journals THE ROLE OF MATRIX TABLET IN DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (1) ◽  
pp. 1 ◽  
Author(s):  
Nita Mondal
Keyword(s):  
Controlled Release ◽  
Safety Margin ◽  
Oral Route ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
The Matrix ◽  
Potent Drug ◽  
Materials Used

Matrix tablet is an important tool for controlled and sustained release dosage forms. The oral route remains the most common route for the administration of drugs. Tablets offer the lowest cost approach to sustained and controlled release dosage forms. The hydrophilic polymer matrix is widely used in this dosage form. The use of different polymers in controlling the release of drugs has become the most important tool in the formulation of matrix tablets. The drug releases by both dissolution-controlled as well as diffusion-controlled mechanisms from the matrix. The development of oral controlled release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. There are several advantages of matrix devices including improved patient compliance due to less frequent drug administration, reduction of fluctuation in steady-state drug levels, maximum utilization of the drug, increased safety margin of a potent drug. This review aims on the discussion of different materials used to prepare matrix tablets, different types of matrix tablets and the drug release mechanism from the matrices.

scholarly journals PHARMACOKINETIC STUDY OF MATRIX MEMBRANE MODERATED TRANSDERMAL SYSTEM OF BOSENTAN MONOHYDRATE

2017 ◽  
Vol 10 (9) ◽  
pp. 255
Author(s):  
Revathi Mannam ◽  
Indira Muzib Yallamalli
Keyword(s):  
Controlled Release ◽  
High Performance ◽  
Release Kinetics ◽  
Research Work ◽  
Fold Increase ◽  
Oral Route ◽  
Fickian Diffusion ◽  
Pharmacokinetic Studies ◽  
The Matrix

Objective: The objective of the present research work is to carry out the pharmacokinetic studies of optimized matrix membrane moderatedtransdermal patch of bosentan monohydrate.Materials and Methods: The matrix membrane moderated transdermal system was formulated using HPMC, HPMC K4M and E RLPO. In vitrodiffusion studies were carried out using modified Franz diffusion cell and for the optimized transdermal patch, pharmacokinetic studies were carriedout using New Zealand male rabbits. Plasma samples were quantified using high-performance liquid chromatography.Results: The in vitro diffusion studies revealed that formulation F3 with HPMC K4M and E RLPO had controlled release up to 28 hrs, and a maximumof 95.02±2.68% drug was released. The release kinetics followed mixed order non-Fickian diffusion. The pharmacokinetic studies of the optimizedpatch revealed controlled release up to 45 hrs where a 2.2-fold increase in area under curve (AUC) and 3.8 times increase in mean residence time(MRT) were observed compared to oral route. The results were appeared to be significant at p≤0.05. The variation in half-life was found to be notstatistically significant when compared between oral and transdermal routes.Conclusion: The pharmacokinetic results concluded that the matrix membrane moderated transdermal system with extended AUC and MRT canenhance the bioavailability of bosentan monohydrate by minimizing the drug-related side effects in oral route.

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