Bioadhesive Mannosylated Nanoparticles for Oral Drug Delivery

2006 ◽  
Vol 6 (9) ◽  
pp. 3203-3209 ◽  
Author(s):  
Hesham H. Salman ◽  
Carlos Gamazo ◽  
Miguel A. Campanero ◽  
Juan M. Irache
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Oral Drug Delivery ◽  
Normal Mucosa ◽  
Oral Drug ◽  
Con A ◽  
Distribution Profile ◽  
The Given

The aim of this work was to design mannosylated Gantrez® AN nanoparticles (M-NP) and to describe their gut bioadhesive properties in order to develop a promising carrier for future applications in oral drug delivery. For that purpose, the process of the nanoparticles coating with mannosamine was optimized by the incubation of Gantrez® AN nanoparticles with different volumes of mannosamine aqueous solutions at different times. Then, the nanoparticles were characterized by measuring the size, zeta potential, mannosamine content, and concanavalin A (Con A) binding. Furthermore, in vivo quantitative bioadhesion study and kinetic analysis of the bioadhesion curves were performed after oral administration to rats of fluorescently labelled nanoparticles. The selected mannosylated nanoparticles (M-NP1 and M-NP10) were of homogenous sizes (about 300 and 200 nm), negatively charged and successfully coated with 36 and 18 μg mannosamine/mg NP, respectively. In vitro agglutination assay using Con A confirmed the successful coating of nanoparticles with mannosamine. The gut distribution profile of M-NP1 indicated a stronger bioadhesive capacity than M-NP10 and non-mannosylated ones, 1 h post-administration. Interestingly, M-NP1 showed an important ileum tropism where around 20% of the given dose remained adhered. Besides, the kinetic parameters of the bioadhesion profile of M-NP1 indicated their higher bioadhesive capacity with Qmax and AUCadh about 2-times higher than control ones. Moreover, fluorescence microscopy corroborated the stronger interactions of M-NP1 with the normal mucosa and demonstrated a strong uptake of these carriers by Peyer's patches. In conclusion, we propose that mannosylated nanoparticles could be a promising non-live vector for oral delivery strategies.

Gastroretentive Microspheres: An Innovative Approach for Prolonging Gastric Residence

2019 ◽  
Vol 9 (01) ◽  
pp. 01-09
Author(s):  
Satyajit Panda ◽  
K Priyanka ◽  
R Varaprasad ◽  
Snigdha Pattnaik
Keyword(s):  
Drug Delivery ◽  
Oral Delivery ◽  
Dosage Form ◽  
Oral Drug Delivery ◽  
Extended Period ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Gastro Retentive

Gastro-retentive drug delivery systems (GRDDS) like gastro-retentive microspheres have gained immense popularity in the field of oral drug delivery. It is a widely employed approach to retain the dosage form in the stomach for an extended period of time and release the drug slowly that can address many challenges associated with conventional oral delivery, including poor bioavailability. Different innovative approaches like magnetic field assisted gastro-retention, swelling systems, mucoadhesion techniques, floating systems with or without effervescence are being applied to fabricate gastroretentive microspheres. Apart from in-vitro characterization, successful gastro-retentive microspheres development demands well designed in-vivo study to establish enhanced gastro-retention and prolonged drug release. Gama scintigraphy and MRI are popular techniques to evaluate in-vivo gastric residence time. However, checking of their overall in-vivo efficacy still remains a major challenge for this kind of dosage form, especially in small animals like mice or rat. Reported in-vivo studies with beagle dogs, rabbits, and human subjects are only a handful in spite of a large number of encouraging in-vitro results. In spite of the many advantages, high subject variations in gastrointestinal physiological condition, effect of food, and variable rate of gastric emptying time are the challenges that limit the availability of gastro-retentive microspheres in the market.

scholarly journals In Vitro and In Vivo Test Methods for the Evaluation of Gastroretentive Dosage Forms

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 416 ◽  
Author(s):  
Schneider ◽  
Koziolek ◽  
Weitschies
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Test Methods ◽  
Delivery Systems ◽  
Oral Drug ◽  
Gastrointestinal Physiology ◽  
In Vivo Test

More than 50 years ago, the first concepts for gastroretentive drug delivery systems were developed. Despite extensive research in this field, there is no single formulation concept for which reliable gastroretention has been demonstrated under different prandial conditions. Thus, gastroretention remains the holy grail of oral drug delivery. One of the major reasons for the various setbacks in this field is the lack of predictive in vitro and in vivo test methods used during preclinical development. In most cases, human gastrointestinal physiology is not properly considered, which leads to the application of inappropriate in vitro and animal models. Moreover, conditions in the stomach are often not fully understood. Important aspects such as the kinetics of fluid volumes, gastric pH or mechanical stresses have to be considered in a realistic manner, otherwise, the gastroretentive potential as well as drug release of novel formulations cannot be assessed correctly in preclinical studies. This review, therefore, highlights the most important aspects of human gastrointestinal physiology and discusses their potential implications for the evaluation of gastroretentive drug delivery systems.

Stearic Acid-g-chitosan Polymeric Micelle for Oral Drug Delivery: In Vitro Transport and in Vivo Absorption

2010 ◽  
Vol 8 (1) ◽  
pp. 225-238 ◽  
Author(s):  
Hong Yuan ◽  
Lin-Juan Lu ◽  
Yong-Zhong Du ◽  
Fu-Qiang Hu
Keyword(s):  
Drug Delivery ◽  
Stearic Acid ◽  
Oral Drug Delivery ◽  
Polymeric Micelle ◽  
Oral Drug ◽  
In Vivo Absorption

In vitro and in vivo studies of enzyme-digestible hydrogels for oral drug delivery

1992 ◽  
Vol 19 (1-3) ◽  
pp. 131-144 ◽  
Author(s):  
Waleed S.W. Shalaby ◽  
William E. Blevins ◽  
Kinam Park
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
In Vivo Studies ◽  
Oral Drug

scholarly journals Self-Nano-Emulsifying Drug-Delivery Systems: From the Development to the Current Applications and Challenges in Oral Drug Delivery

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1194
Author(s):  
Aristote B. Buya ◽  
Ana Beloqui ◽  
Patrick B. Memvanga ◽  
Véronique Préat
Keyword(s):  
Drug Delivery ◽  
Patient Compliance ◽  
Oral Delivery ◽  
Drug Delivery Systems ◽  
Water Solubility ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Statistical Design Of Experiments

Approximately one third of newly discovered drug molecules show insufficient water solubility and therefore low oral bio-availability. Self-nano-emulsifying drug-delivery systems (SNEDDSs) are one of the emerging strategies developed to tackle the issues associated with their oral delivery. SNEDDSs are composed of an oil phase, surfactant, and cosurfactant or cosolvent. SNEDDSs characteristics, their ability to dissolve a drug, and in vivo considerations are determinant factors in the choice of SNEDDSs excipients. A SNEDDS formulation can be optimized through phase diagram approach or statistical design of experiments. The characterization of SNEDDSs includes multiple orthogonal methods required to fully control SNEDDS manufacture, stability, and biological fate. Encapsulating a drug in SNEDDSs can lead to increased solubilization, stability in the gastro-intestinal tract, and absorption, resulting in enhanced bio-availability. The transformation of liquid SNEDDSs into solid dosage forms has been shown to increase the stability and patient compliance. Supersaturated, mucus-permeating, and targeted SNEDDSs can be developed to increase efficacy and patient compliance. Self-emulsification approach has been successful in oral drug delivery. The present review gives an insight of SNEDDSs for the oral administration of both lipophilic and hydrophilic compounds from the experimental bench to marketed products.

Food Protein Based Core–Shell Nanocarriers for Oral Drug Delivery: Effect of Shell Composition on in Vitro and in Vivo Functional Performance of Zein Nanocarriers

2017 ◽  
Vol 14 (3) ◽  
pp. 757-769 ◽  
Author(s):  
Mohammed S. Alqahtani ◽  
M. Saiful Islam ◽  
Satheesh Podaralla ◽  
Radhey S. Kaushik ◽  
Joshua Reineke ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Functional Performance ◽  
Oral Drug ◽  
Core Shell ◽  
Food Protein ◽  
Shell Composition

FLOATING DRUG DELIVERY SYSTEM: A REVIEW

2021 ◽  
pp. 33-39
Author(s):  
Archana Tomar ◽  
Arpita Singh ◽  
Amresh Gupta ◽  
Satyawan Singh
Keyword(s):  
Drug Delivery ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Delivery Systems ◽  
Oral Drug ◽  
Pharmaceutical Dosage Form ◽  
Floating Drug Delivery ◽  
Floating Drug Delivery System

The main motto of working on that article on floating drug delivery systems (FDDS) is to make a compiled report on the recent studies and research with special consideration on the principle mechanism of flotation to achieve gastric retention. The scientific and technological advancements were made in the last few years in the research and development of rate-controlled oral drug delivery systems by overcoming physiological difficulties, like short gastric residence times (GRT) and unpredictable gastric emptying times (GET). This review also epitomized the in-vitro procedure, in-vivo to assess the pursuance and implementation of floating systems, and applications of these systems. These methods are useful to various queries experienced during the development of a pharmaceutical dosage form.

Absence of in vivo–in vitro correlation in per-oral drug delivery

2014 ◽  
Vol 180 ◽  
pp. 150 ◽  
Author(s):  
Kinam Park
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Per Oral
Sign in / Sign up

Export Citation Format

Share Document