scholarly journals Scrutinizing the Feasibility of Nonionic Surfactants to Form Isotropic Bicelles of Curcumin: a Potential Antiviral Candidate Against COVID-19

2021 ◽  
Vol 23 (1) ◽  
Author(s):  
Dina B. Mahmoud ◽  
Mohamed Mofreh Bakr ◽  
Ahmed A. Al-karmalawy ◽  
Yassmin Moatasim ◽  
Ahmed El Taweel ◽  
...  
Keyword(s):  
Oral Delivery ◽  
Mixed Micelles ◽  
Oral Drug Delivery ◽  
Ex Vivo ◽  
Tween 80 ◽  
Pluronic F127 ◽  
Oral Drug ◽  
Simple Method ◽  
Oral Drug Delivery System ◽  
Preclinical And Clinical Studies

AbstractInvestigating bicelles as an oral drug delivery system and exploiting their structural benefits can pave the way to formulate hydrophobic drugs and potentiate their activity. Herein, the ability of non-ionic surfactants (labrasol®, tween 80, cremophore EL and pluronic F127) to form curcumin loaded bicelles with phosphatidylcholine, utilizing a simple method, was investigated. Molecular docking was used to understand the mechanism of bicelles formation. The % transmittance and TEM exhibited bicelles formation with labrasol® and tween 80, while cremophor EL and pluronic F127 tended to form mixed micelles. The surfactant-based nanostructures significantly improved curcumin dissolution (99.2 ± 2.6% within 10 min in case of tween 80-based bicelles) compared to liposomes and curcumin suspension in non-sink conditions. The prepared formulations improved curcumin ex vivo permeation over liposomes and drug suspension. Further, the therapeutic antiviral activity of the formulated curcumin against SARS-CoV-2 was potentiated over drug suspension. Although both Labrasol® and tween 80 bicelles could form bicelles and enhance the oral delivery of curcumin when compared to liposomes and drug suspension, the mixed micelles formulations depicted superiority than bicelles formulations. Our findings provide promising formulations that can be utilized for further preclinical and clinical studies of curcumin as an antiviral therapy for COVID-19 patients.

Thiolated Eudragit-Coated Chitosan Microspheres as an Oral Drug Delivery System

2007 ◽  
Vol 342-343 ◽  
pp. 445-448 ◽  
Author(s):  
Ji Shan Quan ◽  
Hu Lin Jiang ◽  
Yun Jaie Choi ◽  
Mi Kyong Yoo ◽  
Chong Su Cho
Keyword(s):  
Oral Delivery ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Oral Drug ◽  
Average Particle ◽  
Protein Drug ◽  
Chitosan Microspheres ◽  
Oral Drug Delivery System ◽  
Cysteine Hydrochloride

The aim of this study is to prepare mucoadhesive chitosan microspheres for protein drug to deliver to intestine through oral administration. The thiolated Eudragit was synthesized by reaction between L-cysteine hydrochloride and Eudragit® L-100. About 8 mol-% of cysteine was introduced to the Eudragit-cysteine conjugate. The conjugate was used to coat bovine serum albumin (BSA)-loaded chitosan microspheres. The average particle sizes of BSA-loaded thiolated Eudragit-coated chitsoan microspheres (TECMs) were 4.06±0.74 .m and the uniform sizedistribution was shown. The in vitro release of BSA from BSA-loaded TECMs was pH-dependent. Our results indicated that thiolated Eudragit might be a good candidate as a coating material for oral delivery of protein drug owing to mucoadhesive and pH-sensitive properties.

scholarly journals Chitosan-Based Oral Drug Delivery System for Peptide, Protein and Vaccine Delivery

2021 ◽  
Author(s):  
Siti Zuhairah Zainuddin ◽  
Khuriah Abdul Hamid
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Physicochemical Characteristics ◽  
Chemical Diversity ◽  
Oral Drug ◽  
Oral Drug Delivery System ◽  
Orally Active ◽  
Intestinal Efflux

Oral delivery is the most common and preferred route of drug administration due to its convenience and ease of administration. However, various factors such as poor solubility, low dissolution rate, stability, and bioavailability of many drugs remain an ongoing challenge in achieving desired therapeutic levels. The delivery of drugs must overcome various obstacles, including the acidic gastric environment, the presence of the intestinal efflux and influx transporters and the continuous secretion of mucus that protects the gastrointestinal tract (GIT). As the number and chemical diversity of drugs has increased, various strategies are required to develop orally active therapeutics. One of the approaches is to use chitosan as a carrier for oral delivery of peptides, proteins as well as vaccines delivery. Chitosan, a non-toxic N-deacetylated derivative of chitin appears to be under intensive progress during the last years towards the development of safe and efficient chitosan-based drug delivery systems. This polymer has been recognised as a versatile biomaterial because of its biodegradability, biocompatibility, and non-toxicity. This chapter reviews the physicochemical characteristics of chitosan and the strategies that have been successfully applied to improve oral proteins, peptides, and vaccines bioavailability, primarily through various formulation strategies.

Fat-Soluble Vitamins Release Based on Clinoptilolite Zeolite as an Oral Drug Delivery System

2012 ◽  
Vol 9 (2) ◽  
pp. 213-217 ◽  
Author(s):  
Mehdi Rahimi ◽  
Hamid Mobedi ◽  
Aliasghar Behnamghader ◽  
Alireza Nateghi Baygi ◽  
Houri Mivehchi ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Oral Drug Delivery System ◽  
Clinoptilolite Zeolite ◽  
Fat Soluble Vitamins

scholarly journals Mesoporous Carbon: A Versatile Material for Scientific Applications

2021 ◽  
Vol 22 (9) ◽  
pp. 4498
Author(s):  
Md. Motiar Rahman ◽  
Mst Gulshan Ara ◽  
Mohammad Abdul Alim ◽  
Md. Sahab Uddin ◽  
Agnieszka Najda ◽  
...  
Keyword(s):  
Mesoporous Carbon ◽  
Oral Drug Delivery ◽  
High Surface ◽  
High Surface Area ◽  
Oral Drug ◽  
Energy Storage Devices ◽  
Storage Devices ◽  
Catalytic Support ◽  
Scientific Disciplines ◽  
Oral Drug Delivery System

Mesoporous carbon is a promising material having multiple applications. It can act as a catalytic support and can be used in energy storage devices. Moreover, mesoporous carbon controls body’s oral drug delivery system and adsorb poisonous metal from water and various other molecules from an aqueous solution. The accuracy and improved activity of the carbon materials depend on some parameters. The recent breakthrough in the synthesis of mesoporous carbon, with high surface area, large pore-volume, and good thermostability, improves its activity manifold in performing functions. Considering the promising application of mesoporous carbon, it should be broadly illustrated in the literature. This review summarizes the potential application of mesoporous carbon in many scientific disciplines. Moreover, the outlook for further improvement of mesoporous carbon has been demonstrated in detail. Hopefully, it would act as a reference guidebook for researchers about the putative application of mesoporous carbon in multidimensional fields.

scholarly journals Fenofibrate Nanocrystal Composite Microparticles for Intestine-Specific Oral Drug Delivery System

2019 ◽  
Vol 12 (3) ◽  
pp. 109 ◽  
Author(s):  
Bhavesh D. Kevadiya ◽  
Liang Chen ◽  
Lu Zhang ◽  
Midhun B. Thomas ◽  
Rajesh N. Davé
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Imaging System ◽  
Oral Drug ◽  
Burst Release ◽  
Particle Engineering ◽  
Oral Drug Delivery System ◽  
Innovative Idea ◽  
Fast Dissolution ◽  
A Site

Hydrophobic drug nanocrystals (NCs) manufactured by particle engineering have been extensively investigated for enhanced oral bioavailability and therapeutic effectiveness. However, there are significant drawbacks, including fast dissolution of the nanocrystals in the gastric environment, leading to physicochemical instability. To solves this issue, we developed an innovative technique that involves the encapsulation of nanocrystals in composite spherical microparticles (NCSMs). Fenofibrate (FNB) NCs (FNB-NCs) manufactured by a wet stirred media milling (WSMM) technique and an ionotropic crosslinking method were used for FNB-NC encapsulation within gastroresistant NCSMs. Various solid-state methods were used for characterizing NCSMs. The pH-sensitive NCSMs showed a site-specific release pattern at alkaline pH and nearly 0% release at low pH (gastric environment). This phenomenon was confirmed by a real-time in situ UV-imaging system known as the surface dissolution imager (SDI), which was used to monitor drug release events by measuring the color intensity and concentration gradient formation. All these results proved that our NCSM approach is an innovative idea in oral drug delivery systems, as it resolves significant challenges in the intestine-specific release of hydrophobic drugs while avoiding fast dissolution or burst release.

scholarly journals FORMULATION AND CHARACTERIZATION OF LAFUTIDINE NANOSUSPENSION FOR ORAL DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (2) ◽  
pp. 20 ◽  
Author(s):  
Noor Mohammed Dawood ◽  
Shaimaa Nazar Abdal-hammid ◽  
Ahmed Abbas Hussien
Keyword(s):  
Particle Size ◽  
Fourier Transforms ◽  
Oral Drug Delivery ◽  
In Vitro Release ◽  
Tween 80 ◽  
Precipitation Method ◽  
Oral Drug ◽  
Tween 20 ◽  
Dissolution Profile ◽  
Particle Size Reduction

Objective: The objective of this study was to prepare nanosuspension of a practical water insoluble antiulcer drug which is lafutidine to enhance the solubility, dissolution rate with studying the effect of different formulation variables to obtain the best formula with appropriate physical properties and higher dissolution rate.Methods: Nanosuspension of lafutidine was prepared using solvent anti-solvent precipitation method using Polyvinylpyrrolidone K-90(PVP K-90) as the stabilizer. Ten formulations were prepared to show the effect of different variables in which two formulations showed the effect of stabilizer type, three formulations showed the effect of stabilizer concentration, two formulations showed the effect of combination of polymer with surfactant such as tween 80, three formulations show the effect of stirring speed and three formulations prepare to show the effect of addition of co-surfactant such as tween 20. All these formulations are evaluated for their particle size and entrapment efficiency and in vitro release. The selected one was evaluated for zeta potential, scanning electron microscope, atomic force microscopy, Fourier transforms infrared spectroscopy, differential scanning calorimetry, saturation solubility and stability study.Results: The formulations (F3-F10) were in the nano size. The optimum concentration of the stabilizer was in the formulation when the drug: polymer: surfactant ratio 1:4:4 and the optimum stirring speed was 1500 rpm. Dramatic effect on the particle size reduction was found by the addition of co-surfactant (tween 20) in formulation F7 that has a particle size 15.89±1.8 nm. The selected formula F7 showed an enhanced dissolution profile (10 min) compared to the pure drug at all-time intervals.Conclusion: The results show that the formulation that contains drug: PVP-K90: tween 80: tween 20 in ratio 1:4:2:2 is the best one and can be utilized to formulate lafutidine nanosuspension. 

scholarly journals FORMULATION AND EVALUATION OF ATORVASTATIN CALCIUM NANOCRYSTALS CONTAINING P-GLYCOPROTEIN INHIBITORS FOR ENHANCING ORAL DELIVERY

2021 ◽  
pp. 19-23
Author(s):  
SARAH LABIB ◽  
MOHAMED NASR ◽  
MOHAMED NASR
Keyword(s):  
Polyethylene Glycol ◽  
Oral Drug Delivery ◽  
Tween 80 ◽  
Degree Of Crystallinity ◽  
Oral Drug ◽  
Tween 20 ◽  
Atorvastatin Calcium ◽  
Peg 400 ◽  
P Glycoprotein ◽  
Saturated Solubility

Objective: The main objective of this study was to develop atorvastatin calcium (ATR) as an oral drug delivery system for a P-glycoprotein (P-gp) substrate drug using different pharmaceutical excipients that inhibit P-glycoprotein and evaluate the influence of nanocrystals on the dissolution characteristics and bioavailability compared to the plain drug. Methods: A nanosuspension was prepared by Solvent-antisolvent precipitation method using a solvent containing stabilizer that act as a p-gp inhibitor dissolved in distilled water as polyethylene glycol 300, polyethylene glycol 400 (PEG 300, PEG 400), tween 20 and tween 80 while the solvent selected for atorvastatin calcium was methanol. The concentrations were as follows: PEG 300 and 400 = 0.25% w/v, tween 20 and 80 = 0.75% v/v. Nanocrystals were extracted from the suspension and characterized. Results: Particle size of the drug was 1307±127.79 nm while the formulas prepared ranged from 223±17.67 to 887±58.12 nm. Pure ATR had a saturated solubility of 0.059±0.005 mg/ml and the prepared nanocrystals ranged from 0.32±0.021 to 0.88±0.019 mg/ml. The Percentage of drug released of plain atorvastatin calcium reached 41.49% while the formula ranged from 44.32 to 61.5%. Both XRD and SEM discussed the degree of crystallinity as follows: F1<F2<F4<F3<ATR. Conclusion: 0.3% of PEG 300 and PEG 400 were not enough to formulate proper nanocrystals while 0.75% tween 20 and tween 80 achieved acceptable formulas. F4 which is prepared with tween 80 exhibited the highest enhancement in saturated solubility, dissolution rate and subsequently expected to have improved oral bioavailability.

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