Chronomodulated Drug Delivery System of Salmeterol Fluticasone Nlcs Loaded Tablets: Preparation, Characterization, Stability and Drug Release Studies for Management of Asthma

2021 ◽  
Vol 11 (2) ◽  
pp. 95-102
Author(s):  
Mohammed Waseem A ◽  
Ajin P Kurian ◽  
Dhanapal Y
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
Drug Loading ◽  
Water Soluble ◽  
Size Analysis ◽  
Differential Scanning Calorimetric ◽  
Time Interval

Objective: The purpose of this study was to develop salmeterol, fluticasone nano-lipid carriers to estimate as potentials of oral delivery system for poorly water soluble drugs. Nano-lipid carriers applied to chronomodulated pulsatile drug delivery system maintain the concentration level by releasing the drug at predetermined time interval throughout the management of asthma. Method: The particle size analysis revealed that all the formulations were within the nanometer range of 150.0±2.4nm. Percentage of entrapment efficiency and drug loading were found to be 69.5±4.4 - 85.3±1.3 and 9.358±2.2-10.45±8.1, respectively. The SLM-FCN nano-lipid carrier’s optimized formulation showed spherical morphology with smooth surface under the transmission electron microscope (TEM), the crystalline characterization of drug in NLC was investigated by X-ray diffraction and differential scanning calorimetric (DSC). The ex-vivo permeation study showed many folds increment in the SLM-FCN NLCs compared to powder SLM-FCN 96.0±2.55 and pulsing plugs in-vivo drug released effectively in pre-determine time intervals. Conclusion: The progression concludes that chronomodulated programming pulsatile release was achieved with modified pulsing bilayerd plugged of salmeterol, fluticasone propionate NLCs, formulation remarkably improved oral bioavailability. we promise that finding in this investigations suggest practicability of the dosage form system can be taken after at bedtime then it will be delivered in the early morning which maintains the drug concentration throughout to control asthma.

scholarly journals Development of Piperine-Loaded Solid Self-Nanoemulsifying Drug Delivery System: Optimization, In-Vitro, Ex-Vivo, and In-Vivo Evaluation

Nanomaterials ◽  
2021 ◽  
Vol 11 (11) ◽  
pp. 2920
Author(s):  
Ameeduzzafar Zafar ◽  
Syed Sarim Imam ◽  
Nabil K. Alruwaili ◽  
Omar Awad Alsaidan ◽  
Mohammed H. Elkomy ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vitro Release ◽  
System Optimization ◽  
Globule Size

Hypertension is a cardiovascular disease that needs long-term medication. Oral delivery is the most common route for the administration of drugs. The present research is to develop piperine self-nanoemulsifying drug delivery system (PE-SNEDDS) using glyceryl monolinoleate (GML), poloxamer 188, and transcutol HP as oil, surfactant, and co-surfactant, respectively. The formulation was optimized by three-factor, three-level Box-Behnken design. PE-SNEDDs were characterized for globule size, emulsification time, stability, in-vitro release, and ex-vivo intestinal permeation study. The optimized PE-SNEDDS (OF3) showed the globule size of 70.34 ± 3.27 nm, percentage transmittance of 99.02 ± 2.02%, and emulsification time of 53 ± 2 s Finally, the formulation OF3 was transformed into solid PE-SNEDDS (S-PE-SNEDDS) using avicel PH-101 as adsorbent. The reconstituted SOF3 showed a globule size of 73.56 ± 3.54 nm, PDI of 0.35 ± 0.03, and zeta potential of −28.12 ± 2.54 mV. SEM image exhibited the PE-SNEDDS completely adsorbed on avicel. Thermal analysis showed the drug was solubilized in oil, surfactant, and co-surfactant. S-PE-SNEDDS formulation showed a more significant (p < 0.05) release (97.87 ± 4.89% in 1 h) than pure PE (27.87 ± 2.65% in 1 h). It also exhibited better antimicrobial activity against S. aureus and P. aeruginosa and antioxidant activity as compared to PE dispersion. The in vivo activity in rats exhibited better (p < 0.05) antihypertensive activity as well as 4.92-fold higher relative bioavailability than pure PE dispersion. Finally, from the results it can be concluded that S-PE-SNEDDS might be a better approach for the oral delivery to improve the absorption and therapeutic activity.

scholarly journals Formulation and evaluation of solid self micro emulsifying drug delivery system using aerosil 200 as solid carrier

2012 ◽  
Vol 1 (12) ◽  
pp. 414-419 ◽  
Author(s):  
Durgacharan Arun Bhagwat ◽  
John Intru D’Souza
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Intestinal Permeability ◽  
Delivery System ◽  
Ex Vivo ◽  
Water Soluble ◽  
Solid Carrier ◽  
Drug Content ◽  
Permeability Study ◽  
Poorly Water Soluble

Improvement of bio-availability of poorly water soluble drugs presents one of the furthermost challenge in drug formulations. One of the most admired and commercially viable formulation approach for this challenge is solid self micro emulsifying drug delivery system (S-SMEDDS). There are many techniques to convert liquid SMEDDS to solid, but an adsorption technique is simple and economic. Hence aim of present study was to develop S-SMEDDS of poorly water soluble drug Telmisartan (TEL) using Aerosil 200 as solid carrier. Liquid SMEDDS was prepared using Acrysol EL 135, Tween 80 and PEG 400 as oil, surfactant and co-surfactant and was converted to S-SMEDDS by adsorbing it on Aerosil 200. Prepared S-SMEDDS was evaluated for flow properties, drug content, reconstitution properties, DSC, SEM, in-vitro drug release and ex-vivo intestinal permeability study. Results showed that prepared S-SMEDDS have good flow property with 99.45 ± 0.02% drug content. Dilution study by visual observation showed that there was spontaneous micro emulsification and no sign of phase separation. Droplet size was found to be 0.34 µm with polydispersity index of 0.25. DSC thermogram showed that crystallization of TEL was inhibited. SEM photograph showed smooth surface of S-SMEDDS with less aggregation. Drug releases from S- SMEDDS were found to be significantly higher as compared with that of plain TEL. Ex-vivo intestinal permeability study revealed that diffusion of drug was significantly higher from S-SMEDDS than that of suspension of plain TEL. Study concluded that S-SMEDDS can effectively formulated by adsorption technique with enhanced dissolution rate and concomitantly bioavailability.DOI: http://dx.doi.org/10.3329/icpj.v1i12.12451 International Current Pharmaceutical Journal 2012, 1(12): 414-419

scholarly journals Synthesis of a novel green carbon dots as a bioimaging agent and a drug delivery system for enhanced antioxidant and antibacterial efficacy

2020 ◽  
Author(s):  
Neeraj Tejwan ◽  
Mousumi Kundu ◽  
Anirudh Sharma ◽  
Joydeep Das ◽  
Parames C Sil
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Carbon Dots ◽  
Radical Scavenging Activity ◽  
Drug Loading ◽  
Radical Scavenging ◽  
Water Soluble ◽  
Root Extract ◽  
Scavenging Activity

Abstract Background Now-a-days, synthesis of carbon dots (CDs) from renewable sources has attracted considerable attention due to their wide spread availability, lower cost, higher aqueous solubility and more biocompatibility. Here, we have synthesized water soluble CDs from the root extract of red Korean ginseng via simple microwave irradiation. The CDs were further loaded with a natural flavonoid, rutin, to check its efficacy as a drug delivery system. Result The CDs showed a size distribution between 1–4 nm and excitation-dependent fluorescence emission, and could be used as a bio-imaging agent.The CDs showed a drug loading content of 14% and a sustained drug release behavior at physiological conditions. CDs showed excellent free radical scavenging activity both in cell free systems and intra-cellular conditions. Besides, loading with the drug further improved the intra-cellular radical scavenging activity. The CDs and the nanohybrids also showed very little toxicity upto the concentration of 100 µg/mL in normal kidney epithelial cells. The CDs and the nanohybrids also showed a dose-dependent antibacterial effect against both gram negative as well as gram positive bacteria. Conclusion Our synthesized green CDs can be considered as a promising candidate for the biomedical applications due to its facile synthesis, low cytotoxicity, excellent fluorescent properties and potential as drug delivery systems.

scholarly journals Development of a self-microemulsifying drug delivery system of domperidone: In vitro and in vivo characterization

2013 ◽  
Vol 63 (2) ◽  
pp. 241-251 ◽  
Author(s):  
Ramesh Jakki ◽  
Muzammil Afzal Syed ◽  
Prabhakar Kandadi ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Bioavailability ◽  
Ternary Phase Diagram ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Size Analysis

The main objective of this work was to prepare a self-micro emulsifying drug delivery system (SMEDDS) for enhancement of oral bioavailability of domperidone, a poorly water soluble drug. The solubility of the drug was determined in various vehicles. A pseudo ternary phase diagram was constructed to identify the self-micro emulsification region. The in vitro self-micro emulsification properties and droplet size analysis of SMEDDS were studied following their addition to water under mild agitation. Further, the resultant formulations were investigated for clarity, phase separation, globule size, effect of pH and dilutions (1:100, 1:500, 1:1000) and freeze-thaw stability. The optimized formulation, SMEDDS-B used for in vitro dissolution and bioavailability assessment, contained oil (Labrafac CC, 25 %, m/m), surfactant (Tween 80, 55 %, m/m), and co-surfactant (Transcutol®, 20 %, m/m). The preliminary oral bioavailability of domperidone from SMEDDS was 1.92-fold higher compared to that of domperidone suspension in rats. The AUC0-24 and cmax values were 3.38 ± 0.81 μg h mL-1 and 0.44 ± 0.03 μg mL-1 for SMEDDS-B formulation in comparison with 1.74 ± 0.18 μg h mL-1 and 0.24 ± 0.02 μg mL-1 for domperidone suspension, suggesting a significant increase (p < 0.05) in oral bioavailability of domperidone from SMEDDSS.

Development of self-microemulsifying drug delivery system for oral delivery of poorly water-soluble nutraceuticals

2017 ◽  
Vol 44 (6) ◽  
pp. 895-901 ◽  
Author(s):  
Ankita V. Shah ◽  
Heta H. Desai ◽  
Prajwal Thool ◽  
Damon Dalrymple ◽  
Abu T. M. Serajuddin
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Water Soluble ◽  
Poorly Water Soluble

Formulation and Evaluation of Self-Nanoemulsifying Drug Delivery System of Naproxen

2015 ◽  
Vol 8 (1) ◽  
pp. 2715-2722
Author(s):  
Saritha D ◽  
Penjuri Subhash Chandra Bose ◽  
Nagaraju Ravoru
Keyword(s):  
Drug Delivery ◽  
Oral Administration ◽  
Drug Delivery System ◽  
Delivery System ◽  
Water Soluble ◽  
Size Analysis ◽  
Albino Rats ◽  
Significant Activity ◽  
Water Soluble Drugs

Self-emulsifying drug delivery systems (SEDDS) possess unparalleled potential in improving oral bioavailability of poorly water-soluble drugs. Following their oral administration, these systems rapidly disperse in gastrointestinal fluids, yielding micro or nanoemulsions containing the solubilized drug. The objective of the present work was to formulate a self nanoemulsifying drug delivery system (SNEDDS) for naproxen. Naproxen SNEDDS were formulated using Labrafac PG (Oil), Span 80 (Surfactant) and propylene glycol (Co surfactant). The developed SNEDDS were evaluated for turbidimetry, droplet size analysis, zeta potential, refractive index, viscosity, drug content and in vitro diffusion profiles. All formulations of naproxen SNEDDS showed globule size in nanometric range, good stability with no phase separation and rapidly formed clear emulsion. All formulations showed more than 95% of drug release at the end of 60 min. The SEDDS showed improved dissolution rate compared to pure naproxen. Anti-inflammatory studies were conducted in Wistar strain male albino rats and ibuprofen SNEDDS showed more significant activity than the pure drug. The study illustrated the potential of naproxen SNEDDS for oral administration and its biopharmaceutical performance.

scholarly journals Preparation and Characterization of Self-Microemulsifying Drug Delivery System of Olmesartan Medoxomil for Bioavailability Improvement

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Shailesh T. Prajapati ◽  
Harsh A. Joshi ◽  
Chhaganbhai N. Patel
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Ex Vivo ◽  
Tween 80 ◽  
Olmesartan Medoxomil ◽  
Water Soluble ◽  
Absolute Bioavailability ◽  
Angiotensin Ii Receptor Blocker

Olmesartan medoxomil (OLM) is an angiotensin II receptor blocker (ARB) antihypertensive agent administered orally that has absolute bioavailability of only 26% due to the poor aqueous solubility (7.75 μg/ml). The aim of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the oral absorption of OLM. The solubility of OLM in various oils, surfactants, and cosurfactants was determined. Pseudoternary phase diagrams were constructed using Acrysol EL 135, Tween 80, Transcutol P, and distilled water to identify the efficient self-microemulsification region. Prepared SMEDDS was further evaluated for its emulsification time, drug content, optical clarity, droplet size, zeta potential, in vitro dissolution, and in vitro and ex vivo drug diffusion study. The optimized formulation S2 contained OLM (20 mg), Tween 80 (33%v/v), Transcutol P (33%v/v), and Acrysol EL 135 (34%v/v) had shown the smallest particle size, maximum solubility, less emulsification time, good optical clarity, and in vitro release. The in vitro and ex vivo diffusion rate of the drug from the SMEDDS was significantly higher than that of the plain drug suspension. It was concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.

scholarly journals Development, Characterization, and Pharmacokinetic Evaluation of a CRV431 Loaded Self-Microemulsifying Drug Delivery System

2018 ◽  
Vol 21 (1s) ◽  
pp. 335s-348s ◽  
Author(s):  
Daniel J Trepanier ◽  
Daren R Ure ◽  
Robert Thomas Foster
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Cyclosporine A ◽  
Oral Delivery ◽  
Ternary Phase Diagram ◽  
Drug Loading ◽  
Aqueous Media ◽  
Ionization Mass ◽  
Healthy Human

PURPOSE: The objective of this study was to develop a self-microemulsifying drug delivery system (SMEDDS) formulation for the oral delivery of CRV431, a non-immunosuppressive analogue of cyclosporine A. Relative to cyclosporine A, CRV431 is poorly soluble in lipid solvents and thusly presents a challenge for the development of a formulation of sufficient oral bioavailability for clinical use. METHODS: The solubility of CRV431, a cyclosporine derivative, was determined in a range of commonly used surfactants, oils and co-solvents. A pseudo-ternary phase diagram was constructed from the most soluble excipients and prototype formulations, SERIES 1 and SERIES 2 were developed. The pharmacokinetics, following single oral doses of 1 and 3 mg/kg of CRV431 SMEDDS, was studied in healthy human volunteers using liquid chromatography-electrospray ionization-mass spectrometry (LC-ESI-MS). RESULTS: The maximum drug load for the SERIES 1 formulations was less than 40 mg/ml. Manipulation of the excipient ratios allowed for the development of SERIES 2 formulations, which had higher drug loading capacity and stability for CRV431 compared to SERIES 1. Further improvements allowed for the development of an optimized SMEDDS formulation containing up to 90 mg/ml CRV431 and which generated a microemulsion mean particle size of 25 nm when dispersed into aqueous media. The pharmacokinetics of the optimized CRV431 SMEDDS displayed excellent total body exposure and dose-proportional effects in humans, and high drug levels in the liver of rats. CONCLUSIONS: The developed SMEDDS formulation should allow for effective clinical development of CRV431, targeted to the treatment of liver diseases including hepatitis B (HBV), fibrosis, and hepatocellular carcinoma.

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

2016 ◽  
Vol 8 (11) ◽  
pp. 144
Author(s):  
Suwarna R. Deshmukh ◽  
Suparna S. Bakhle ◽  
Kanchan P. Upadhye ◽  
Gouri R. Dixit
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Water Soluble Drug

Objective: Gliclazide (GCZ) is a widely prescribed anti-diabetic drug belongs to class IΙ under BCS and exhibit low and variable oral bioavailability due to its poor aqueous solubility. The present investigations highlight the development of solid self-emulsifying drug delivery system (solid-SEDDS) for improved oral delivery of the poorly water-soluble drug, GCZ.Methods: Various oils, surfactant and co-surfactant, were screened for their emulsification ability. Ternary phase diagrams were plotted to identify the zone of micro-emulsification. Liquid SEDDS of the drug were formulated using lemon oil as the oil phase, tween 80, as the surfactant, and labrasol, as the co-surfactant. The optimized liquid SEDDS was transformed into free-flowing powder using florite R as the adsorbent. Results: Self-emulsifying powder retained the self-emulsifying property of the liquid SEDDS. The morphology of solid-SEDDS from scanning electron microscopy studies demonstrated the presence of spherical, granular particles indicating good flowing ability. X-ray powder diffraction studies confirmed solubilization of the drug in the lipid excipients and/or transformation of a crystalline form of the drug to amorphous form. In vitro dissolution studies revealed enhanced release of the drug from solid-SEDDS as compared to plain drug and marketed formulation.Conclusion: Thus it can be concluded that solid-SEDDS, amenable for the development of solid dosage form, can be successfully developed using florite R with the potential of enhancing the solubility, dissolution rate, and bioavailability of the drug.

Improved Oral Delivery of Rosuvastatin by Using Self Nanoemulsifying Drug Delivery System

2013 ◽  
Vol 678 ◽  
pp. 286-290 ◽  
Author(s):  
N. Subramanian ◽  
P. Chandra Sekar ◽  
S. Abimanyu ◽  
S.P. Sharavanan ◽  
R. Gayathri ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Delivery ◽  
Oral Absorption ◽  
Ex Vivo ◽  
Lipid Lowering ◽  
Conventional Tablet

The aim of the present study was to develop a self nanoemulsifying drug delivery system (SNEDDS) for the improved oral delivery of Rosuvastatin, a lipid lowering agent. Captex 810D, based on the higher solubility of Rosuvastatin was selected as an oil phase. Mixture of permeation enhancers such as Solutol HS15 and Acconon MC8 was selected as surfactants for the formulation of SNEDDS. Formulated SNEDDS upon mixing with water, dispersed rapidly into fine droplets size ranging from 95-263nm. Further the SNEDDS was evaluated for self nanoemulsification time, precipitation, cloud point, morphology, in-vitro drug release and ex-vivo permeation. Formulation (F3) showed the globule size of 139nm, quick self nanoemulsifiation time (20 sec) and transparency (97%). Maximum drug release of 99.9% and higher drug permeation of 95% was observed with formulation F3 when compared with conventional tablet. The formulated SNEDDS can be used to improve the oral absorption and bioavailability of Rosuvastatin.

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