scholarly journals EUDRAGIT COATED ALGINATE BEADS BEARING OXALIPLATIN LOADED LIPOSOMES: FORMULATION, OPTIMIZATION AND IN VITRO CHARACTERIZATION

2021 ◽  
pp. 170-177
Author(s):  
ANKITA TIWARI ◽  
SANJAY K. JAIN
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Alginate Beads ◽  
Molar Ratio ◽  
Specific Drug ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Vesicle Size

Objective: The present investigation aimed to develop and characterize Eudragit S-100 coated alginate beads bearing oxaliplatin loaded liposomes for colon-specific drug delivery. Methods: Liposomes were formulated by the thin-film hydration method. The process and formulation variables were optimized by Box-Behnken design (BBD) with the help of Design-Expert® Software. Three independent variables taken were HSPC: Chol molar ratio (X1), hydration time (X2), and sonication time (X3). The response variables selected were entrapment efficiency of oxaliplatin, polydispersity index, and vesicle size. Results: The liposomes possessed an average vesicle size of 110.1±2.8 nm, PDI 0.096±0.3, zeta potential of-6.70±1.4 mV, and entrapment efficiency of 27.65%. The beads were characterized for their size, in vitro drug release, and swelling index. The degree of swelling of the beads was found to be 2.3 fold higher at pH 7.4 than at pH 1.2. The in vitro drug release depicted a sustained drug release in 48 h. Conclusion: The outcomes of the study proposed that the developed system can be effectively used for site-specific drug delivery to the colon via the oral route.

scholarly journals Development and In-Vitro Evaluation of Budesonide Mucoadhesive Microspherefor Pulmonary Drug Delivery

2021 ◽  
Vol 11 (2-S) ◽  
pp. 76-81
Author(s):  
Jddtadmin Journal
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Chemical Interaction ◽  
Entrapment Efficiency ◽  
Pulmonary Drug Delivery ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Drug Entrapment Efficiency

Thepurpose of the study was to develop and evaluatemucoadhesive microspheres of Budesonide for pulmonary drug delivery systemhaving prolonged residence time and sustained drug release. Microspheres were prepared by emulsificationsolvent evaporation technique using HPMC, carbopol as polymers in varying ratios. The microspheres were evaluated for its percentage yield, drug entrapment efficiency, particle size and shape, in vitro mucoadhesion study and in vitro drug release studies.The FTIR studies revealed no chemical interaction between the drug molecule and polymers and found that drug was compatible with used polymer. The mucoadhesive microspheres showed particle size, drug entrapment efficiency and yield in the ranges of148 - 164 μm, 68.0 - 85.0%and67.52 - 87.25% respectively. In vitro drug release and mucoadhesion study confirms thatformulationF5 was the best formulation as it releases 81.8 % at the end of 12 hr. in controlled manner and percentage mucoadhesion of 75.2 % after 10 hr. This confirms the developed budesonidemucoadhesive microspheres are promising for pulmonary drug delivery system.   Keywords: Budesonide, Mucoadhesion, Microspheres, Drug entrapment efficiency.

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 Steroid Eluting Esophageal-Targeted Drug Delivery Devices for Treatment of Eosinophilic Esophagitis

Polymers ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 557
Author(s):  
Alka Prasher ◽  
Roopali Shrivastava ◽  
Denali Dahl ◽  
Preetika Sharma-Huynh ◽  
Panita Maturavongsadit ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Porcine Model ◽  
Pharmacokinetic Studies ◽  
Specific Drug ◽  
In Vitro Drug Release ◽  
Release Studies ◽  
3D Printed

Eosinophilic esophagitis (EoE) is a chronic atopic disease that has become increasingly prevalent over the past 20 years. A first-line pharmacologic option is topical/swallowed corticosteroids, but these are adapted from asthma preparations such as fluticasone from an inhaler and yield suboptimal response rates. There are no FDA-approved medications for the treatment of EoE, and esophageal-specific drug formulations are lacking. We report the development of two novel esophageal-specific drug delivery platforms. The first is a fluticasone-eluting string that could be swallowed similar to the string test “entero-test” and used for overnight treatment, allowing for a rapid release along the entire length of esophagus. In vitro drug release studies showed a target release of 1 mg/day of fluticasone. In vivo pharmacokinetic studies were carried out after deploying the string in a porcine model, and our results showed a high local level of fluticasone in esophageal tissue persisting over 1 and 3 days, and a minimal systemic absorption in plasma. The second device is a fluticasone-eluting 3D printed ring for local and sustained release of fluticasone in the esophagus. We designed and fabricated biocompatible fluticasone-loaded rings using a top-down, Digital Light Processing (DLP) Gizmo 3D printer. We explored various strategies of drug loading into 3D printed rings, involving incorporation of drug during the print process (pre-loading) or after printing (post-loading). In vitro drug release studies of fluticasone-loaded rings (pre and post-loaded) showed that fluticasone elutes at a constant rate over a period of one month. Ex vivo pharmacokinetic studies in the porcine model also showed high tissue levels of fluticasone and both rings and strings were successfully deployed into the porcine esophagus in vivo. Given these preliminary proof-of-concept data, these devices now merit study in animal models of disease and ultimately subsequent translation to testing in humans.

scholarly journals Formulation and Invitro characterization of Flurbiprofen loaded Nanosponges

2021 ◽  
Vol 12 (3) ◽  
pp. 1798-1802
Author(s):  
Gangadhara R. ◽  
Satheesh K. P. ◽  
Devanna N. ◽  
Sasikala L. ◽  
Vandavasi Koteswara Rao
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Guar Gum ◽  
Entrapment Efficiency ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
Topical Gel ◽  
High Entrapment Efficiency

The aim of this analysis is to see how effective a Nanosponge-loaded topical gel is at distributing flurbiprofen through the skin. Flurbiprofen was entrapped in Nanosponge and formulated into a gel for this purpose. Flurbiprofen Nanosponges were developed by solvent evaporation using pluronic F68 and ethyl cellulose. The particle size and entrapment quality were discovered to be in the range of 200-410 nm and 90.94% to 98.68%, respectively. For gel formulation, Nanopsonges with high entrapment efficiency and the smallest particle size (F3) were chosen based on the characterization. Using Guar gum, Carbopol, and HPMC K4M, a total of 6 formulations were produced to determine the sustained drug release and were tested for physiochemical tests, producing positive results. According to the findings of the above in vitro drug release trials, formulations containing carbopol release more drug at the end of 11 hours than other formulations and follow a zero-order with case II transport mechanism.

scholarly journals Synthesis, in-vitro characterization and pharmacological evaluation of conjugates of flurbiprofen and polysaccharides for colon specific drug delivery

2019 ◽  
Vol 9 (2) ◽  
pp. 316-320
Author(s):  
P Soni ◽  
K Soni ◽  
GP Choudhary
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Specific Drug ◽  
Glycosidic Linkage ◽  
In Vitro Drug Release ◽  
In Vitro Characterization ◽  
Microbial System ◽  
Colon Specific Drug Delivery ◽  
Upper Gastrointestinal

The aim of the study was to prepare site specific drug delivery of flurbiprofen using polysaccharides by the formation of glycosidic linkage which is hydrolysed by the microflora present in colon. This approach prevents drug release in the upper gastrointestinal environment. Due to the minimal degradation of conjugates in upper Git, the in vitro drug release in SGF, SIF and SCF was found upto 4.26±0.03%, 12.41±0.08% and 92.72±3.33% respectively. Keywords: Colon specific drug delivery, Conjugates, Flurbiprofen, Microbial system.

Formulation Design and In-vitro Characterization of Docetaxel Cubosomes for Gastric Cancer therapy

2021 ◽  
pp. 179-184
Author(s):  
P. Rajesh Kumar ◽  
M. Ravinder Nayak ◽  
A. Srinivasa Rao
Keyword(s):  
Drug Release ◽  
Evaluation Studies ◽  
Antineoplastic Agent ◽  
Entrapment Efficiency ◽  
Cubic Phase ◽  
Sustained Drug Release ◽  
In Vitro Drug Release ◽  
In Vitro Characterization ◽  
Ich Guidelines

Cubosomes are altered cubic phase systems, which are emerging as promising drug delivery system for the delivery of both hydrophilic and lipophilic drugs. Docetaxel is an antineoplastic agent that has a unique mechanism of action as an inhibitor of cellular mitosis and that currently plays a central role in the therapy of many solid tumors including breast and lung cancer. Docetaxel in the form of cubosomes. The main aim of present research was to encapsulate, Docetaxel in cubosomes for sustained drug release. Docetaxel loaded cubosomes were prepared by Bottom-Up Method technique using Glyceryl Mono Oleate and pluronic F-127 and Pluronic F68 in different ratios. The prepared formulations were subjected to evaluation studies for excipient compatibility, particle size, drug content, entrapment efficiency and In vitro drug release. The maximum entrapment efficiency was found as 90.15% with, and In vitro drug release as 99.37%. Stability studies were also conducted for the formulations as per protocol mentioned in ICH guidelines. These results suggest that the cubosomal formulation F4 is suitable for the delivery of Docetaxel.

scholarly journals Formulation and In-Vitro Evaluation of Niosomal drug Delivery in Cancer Chemotherapy

2017 ◽  
Vol 5 (04) ◽  
pp. 29-33
Author(s):  
Naresh Kalra ◽  
G. Jeyabalan
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Delivery System ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
The Body ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Ethanol Injection

Drug delivery systems are defined as formulations aim for transportation of a drug to the desired area of action within the body. The aim of the study was to investigate the feasibility of using Niosomes as a drug delivery system for Cisplatin By entrapment of drug in Niosomes, dose also could be reduced. Niosomes were prepared by Ethanol injection method using cholesterol and Surfactant. Particle size, zeta potential, entrapment efficiency and in vitro drug release studies were performed. The targeted niosome delivery system is composed of drug, surfactant and cholesterol. With regard to the influence of formulation variables on the percent drug loading (PDL), different compositions with varying ratios of surfactant and cholesterol were studied. In –Vitro drug release mechanism was studied for 24 hours.

Formulation, Development and Characterization of Floating Beads of Diltiazem Hydrochloride

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.

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.

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