scholarly journals Stomach-Specific Drug Delivery of Clarithromycin Using aSemi Interpenetrating Polymeric Network Hydrogel Made ofMontmorillonite and Chitosan: Synthesis, Characterization and InVitro Drug Release Study

2019 ◽  
Vol 9 (1) ◽  
pp. 159-173 ◽  
Author(s):  
Yunes Panahi ◽  
Afshin Gharekhani ◽  
Hamed Hamishehkar ◽  
Parvin Zakeri-Milani ◽  
Hamed Gharekhani
Keyword(s):  
Drug Delivery ◽  
Hydrochloric Acid ◽  
Drug Release ◽  
Polymer Network ◽  
In Vitro Release ◽  
Extended Period ◽  
Interpenetrating Polymer Network ◽  
Swelling Kinetic ◽  
Hydrogel Nanocomposite

Purpose: In this study, we aimed to prepare an extended drug delivery formulation ofclarithromycin (CAM) based on a semi-interpenetrating polymer network (semi-IPN) hydrogel.Methods: Synthesis of semi-IPN hydrogel nanocomposite made of chitosan (CS), acrylicacid (AA), acrylamide (AAm), polyvinylpyrrolidone (PVP), and montmorillonite (MMT) wasperformed by free radical graft copolymerization method. Swelling kinetic studies were done inacidic buffer solutions of hydrochloric acid (pH = 1.2), acetate (pH = 4), and also distilled water.Also, the effects of MMT on the swelling kinetic, thermal stability, and mechanical strengthof the hydrogels were evaluated. Moreover, in vitro release behavior of CAM and its releasekinetics from hydrogels were studied in a hydrochloric acid buffer solution.Results: Fourier transform infrared spectroscopy (FTIR) results revealed that synthesis of semi-IPN superabsorbent nanocomposite and CAM incorporation into hydrogel was performed,successfully. Introducing MMT into hydrogel network not only improved its thermal stabilitybut also increased mechanical strength of the final hydrogel product. Also, in comparisonwith neat hydrogel (1270 g/g), hydrogel nanocomposite containing 13 wt% MMT exhibitedgreater equilibrium swelling capacity (1568 g/g) with lower swelling rate. In vitro drug releaseexperiments showed that CS-g-poly(AA-co-AAm)/PVP/MMT/CAM formulation possesses asustained release character over extended period of time compared with CS-g-poly(AA-co-AAm)/PVP/CAM formulation.Conclusion: In the presence of MMT, the effective life time of drug is prolonged, demonstrating asustained release property. The reason is that interlinked porous channels within superabsorbentnanocomposite network hinder penetration of aqueous solutions into hydrogel and subsequentlycause a slower drug release.

Design, Synthesis and Studies on Novel Polymeric Prodrugs of Erlotinib for Colon Drug Delivery

2020 ◽  
Vol 20 ◽  
Author(s):  
Sahil Kumar ◽  
Bandna Sharma ◽  
Tilak R. Bhardwaj ◽  
Rajesh K. Singh
Keyword(s):  
Drug Delivery ◽  
Colon Cancer ◽  
Drug Release ◽  
Anticancer Agents ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Specific Treatment ◽  
Drug Conjugates ◽  
Polymer Drug Conjugates

Aims: In the present study, polymer-drug conjugates were synthesized based on azo-bond cleavage drug delivery approach for targeting erlotinib as anticancer drug specifically to the colon for the proficient treatment of colon cancer. Background: Colon cancer (CC) is the third commonly detected tumor worldwide and it make up about 10 % of all cases of cancers. Most of the chemotherapeutic drugs available for treating colon cancer are not only toxic to cancerous cells but also to the normal healthy cells. Among the various approaches to get rid of the adverse effects of anticancer agents, prodrugs are one of the most imperative approaches. Objective: The objective of the study is to chemically modify the erlotinib drug through azo-bond linkage and suitable spacer which will be finally linked to polymeric backbone to give desired polymer linked prodrug. The azo reductase enzyme present in colon is supposed to cleave the azo-bond specifically and augment the drug release at the colon. Methods: The synthesized conjugates were characterized by IR and 1H-NMR spectroscopy. The cleavage of aromatic azobond resulted in a potential colon-specific liberation of drug from conjugate studied in rat fecal contents. In vitro release profiles of polyphosphazene-linked conjugates of erlotinib have been studied at pH 1.2, pH 6.8 and pH 7.4. The stability study was designed to exhibit that free drug was released proficiently and unmodified from polyphosphazene-erlotinib conjugates having aromatic azo-bond in artificial colon conditions. Results: The synthesized conjugates were demonstrated to be stable in simulated upper gastro-intestinal tract conditions. The drug release kinetics shows that all the polymer-drug conjugates of erlotinib follow zero-order release kinetics which indicates that the drug release from the polymeric backbone is independent of its concentration. Kinetic study of conjugates with slope (n) shows the anomalous type of release with an exponent (n) > 0.89 indicating a super case II type of release. Conclusion: These studies indicate that polyphosphazene linked drug conjugates of erlotinib could be the promising candidates for the site-specific treatment of colon cancer with least detrimental side-effects.

scholarly journals Influence of sterilization on the drug release behaviour of drug coated silicone

2021 ◽  
Vol 7 (2) ◽  
pp. 672-675
Author(s):  
Katharina Wulf ◽  
Stefan Raggl ◽  
Thomas Eickner ◽  
Gerrit Paasche ◽  
Niels Grabow
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Polymer Coating ◽  
Drug Loading ◽  
In Vitro Release ◽  
Physical Chemical ◽  
Release Studies ◽  
Vitro Release ◽  
Dual Drug

Abstract Sterilization processes ensure sterility of drug delivery systems, but may negatively affect the properties of biomaterials and incorporated drugs by changing their physical, chemical, mechanical properties and drug release behaviour. Therefore, it is important to investigate their influence. In this study, the influence of ethylene oxide (EtO) sterilization on the drug loading and release behaviour of incorporated Diclofenac (DCF) in a Poly-L-lactide (PLLA) coating and Dexamethasone (DMS) in the silicone carrier is presented. Silicone samples containing DMS were coated with PLLA containing DCF varying in layer thickness (5, 10, and 20 μm). Half of the samples underwent EtO sterilization, the other half was not sterilized. All un-/sterilized sample surfaces were in view of the morphology and hydrophilicity examined. Furthermore, in vitro release studies of DMS and DCF were conducted. The sterilized sample surfaces showed no morphological and hydrophilicity changes. The DCF and DMS loadings were similar for the sterile and untreated samples. This also applied to the in vitro DMS release profiles apart from the end of the studies where slight differences were evident. The results indicate that both drugs loaded in the polymer coating and the silicone were not impaired by the sterilization process. Thus, EtO sterilization appears suitable for DMS containing silicone and DCF incorporated PLLA coatings as a dual drug delivery system.

Formulation and evaluation of resveratrol loaded cubosomal nanoformulation for topical delivery

2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Topical Application ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Drug Permeation

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.

scholarly journals FORMULATION AND EVALUATION OF SELF-EMULSIFYING DRUG DELIVERY SYSTEM OF ETORICOXIB

2017 ◽  
Vol 10 (7) ◽  
pp. 367 ◽  
Author(s):  
Surendra Singh Saurabh ◽  
Roshan Issarani ◽  
Nagori Bp
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
In Vitro Release ◽  
Stability Study ◽  
In Vitro Drug Release ◽  
In Vitro Permeation ◽  
Globule Size ◽  
Vitro Release ◽  
As Solubility

Objective: In the present dissertation work, the aim was to prepare self-emulsifying drug delivery systems (SEDDS) of etoricoxib to improve its solubility with a view to enhance its oral bioavailability.Methods: The prepared SEDDS was the concentrate of drug, oil, surfactants, and cosurfactant. The formulation was evaluated for various tests such as solubility, globule size, thermodynamic stability study, pH determination, ease of dispersibility, uniformity index, drug content, in-vitro release study, and in-vitro permeation study.Results: The optimized formulation F6 showed drug release (79.21±2.73%), droplet size (0.546 μm). In vitro drug release of the F6 was highly significant (p<0.05) as compared to the plain drug.Conclusion: All formulations of etoricoxib SEDDS were showed faster dissolution than plain drug (p<0.05), mean bioavailability of etoricoxib increase in respect to the plain drug. The F6 can be further used for the preparation of various solid SEDDS formulations.

scholarly journals Preparation and In Vitro Evaluation of Aspartic/Alginic Acid Based Semi-Interpenetrating Network Hydrogels for Controlled Release of Ibuprofen

Gels ◽  
2021 ◽  
Vol 7 (2) ◽  
pp. 68
Author(s):  
Muhammad Suhail ◽  
Yi-Han Hsieh ◽  
Arshad Khan ◽  
Muhammad Usman Minhas ◽  
Pao-Chu Wu
Keyword(s):  
Drug Release ◽  
Acrylic Acid ◽  
Aspartic Acid ◽  
Alginic Acid ◽  
Drug Loading ◽  
Polymer Network ◽  
Interpenetrating Polymer Network ◽  
Polymerization Process ◽  
Ph Dependent

Different combinations of polymers, aspartic acid (ASP), alginic acid (AL), and monomer acrylic acid (AA) were crosslinked in the presence of an initiator ammonium peroxodisulfate (APS) and cross-linker ethylene glycol dimethacrylate (EGDMA) to develop aspartic acid/alginic acid-co-poly(acrylic acid) (ASP/ALPAA) (semi-interpenetrating polymer network (SIPN)) hydrogels by the free radical polymerization technique for the controlled delivery of ibuprofen (IBP). Various studies such as dynamic swelling studies, drug loading, in vitro drug release and sol−gel analysis were carried out for the hydrogels. Higher swelling was observed at higher pH 7.4 as compared to lower pH 1.2, due to the presence of carboxylic groups of polymers and the monomer. Hence, pH-dependent swelling was exhibited by the developed hydrogels which led to a pH-dependent drug release and vice versa. The structural properties of the hydrogels were assessed by FTIR, PXRD, TGA, DSC, and SEM which confirmed the fabrication and stability of the developed structure. FTIR analysis revealed the reaction of both polymers with the monomer during the polymerization process and confirmed the overlapping of the monomer on the backbone of the both polymers. The disappearance of high intense crystalline peaks and the encapsulation of the drug by the hydrogel network was confirmed by PXRD. TGA and DSC showed that the developed hydrogels were thermally more stable than their basic ingredients. Similarly, the surface morphology of the hydrogels was analyzed by SEM and showed a smooth surface with few pores. Conclusively, ASP/ALPAA hydrogels have the potential to deliver IBP for a long period of time in a controlled way.

scholarly journals Ethyl Cellulose and Hydroxypropyl Methyl Cellulose Blended Methotrexate-Loaded Transdermal Patches: In Vitro and Ex Vivo

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3455
Author(s):  
Muhammad Shahid Latif ◽  
Abul Kalam Azad ◽  
Asif Nawaz ◽  
Sheikh Abdur Rashid ◽  
Md. Habibur Rahman ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Ex Vivo ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Transdermal Patches ◽  
Percent Moisture ◽  
Vitro Release

Transdermal drug delivery systems (TDDSs) have become innovative, fascinating drug delivery methods intended for skin application to achieve systemic effects. TDDSs overcome the drawbacks associated with oral and parenteral routes of drug administration. The current investigation aimed to design, evaluate and optimize methotrexate (MTX)-loaded transdermal-type patches having ethyl cellulose (EC) and hydroxypropyl methyl cellulose (HPMC) at different concentrations for the local management of psoriasis. In vitro release and ex vivo permeation studies were carried out for the formulated patches. Various formulations (F1–F9) were developed using different concentrations of HPMC and EC. The F1 formulation having a 1:1 polymer concentration ratio served as the control formulation. ATR–FTIR analysis was performed to study drug–polymer interactions, and it was found that the drug and polymers were compatible with each other. The formulated patches were further investigated for their physicochemical parameters, in vitro release and ex vivo diffusion characteristics. Different parameters, such as surface pH, physical appearance, thickness, weight uniformity, percent moisture absorption, percent moisture loss, folding endurance, skin irritation, stability and drug content uniformity, were studied. From the hydrophilic mixture, it was observed that viscosity has a direct influence on drug release. Among all formulated patches, the F5 formulation exhibited 82.71% drug release in a sustained-release fashion and followed an anomalous non-Fickian diffusion. The permeation data of the F5 formulation exhibited about a 36.55% cumulative amount of percent drug permeated. The skin showed high retention for the F5 formulation (15.1%). The stability study indicated that all prepared formulations had very good stability for a period of 180 days. Therefore, it was concluded from the present study that methotrexate-loaded transdermal patches with EC and HPMC as polymers at different concentrations suit TDDSs ideally and improve patient compliance for the local management of psoriasis.

scholarly journals Formulation and evaluation of gastro-retentive floating tablets of terbinafine

2020 ◽  
Vol 13 (1) ◽  
pp. 257-266
Author(s):  
Kapil Jalodiya ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Extended Period ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Gastro Retentive

Gastro-retentive dosage forms enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal tract and improve the bioavailability of medications those are characterized by a narrow absorption window. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of terbinafine were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of terbinafine were evaluated tablet hardness, uniformity of weight, friability, uniformity of content, in vitro buoyancy test, swelling index, in vitro dissolution study and stability study. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of terbinafine shown that the formulation F5 was found to be the best formulation as it releases 96.22% terbinafine in a controlled manner for an extended period of time (up to 480 min). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of terbinafine may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.

scholarly journals Formulation development and evaluation of gastroretentive mucoadhesive tablets of glimepiride using natural polymers

2020 ◽  
Vol 10 (4-s) ◽  
pp. 153-159
Author(s):  
Rahul Malasiya ◽  
Tarkeshwar P. Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Extended Period ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets ◽  
Gastro Retentive

Glimepiride, a third-generation sulfonylurea is poorly soluble anti-diabetic drug. Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipients. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. The development of mucoadhesive sustained release drug delivery system is recommended in order to enhance the bioavailability. A mucoadhesive tablets were developed using the natural polymer sodium alginate and gum tragacanth. Mucoadhesion is a complex phenomenon which involves wetting, adsorption and interpenetration of polymer chains. The tablets of glimepiride were prepared by direct compression method. Pre-compression parameters were evaluated. The tablets were evaluated for post-compression parameters such as thickness, hardness, average weight, friability and In vitro release studies. All the compositions were resulted in adequate pharmacopoeial limits. The varying concentration of polymers was found to affect on in-vitro drug release and mucoadhesive strength. In vitro drug release of gastro retentive tablet of glimepiride shown that the formulation F5 was found to be the best formulation as it releases 98.78%.  Glimepiride in a sustain release manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as higuchi, korsmeyer-peppas, first order and zero order to evaluate the kinetics and mechanism of the drug release. Prepared tablets of glimepiride may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Glimepiride, Gastro retentive, Anti-diabetic drug, Direct compression method

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