Design of a Soft, Self-Uncoiling Stent for Extended Retention of Drug Delivery in the Small Intestine

2020 ◽  
Author(s):  
Sunandita Sarker ◽  
Ryan Jones ◽  
Gabriel Chow ◽  
Benjamin Terry
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Oral Drug Delivery ◽  
Ileocecal Valve ◽  
Drug Carriers ◽  
Oral Formulation ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Biological Drugs

Abstract Despite being the preferred route of drug administration, the oral formulation of biological drugs is limited due to its intrinsic instability, low permeability, and physical, chemical and immunological barriers. Various innovative swallowable technologies such as drug-loaded, dissolvable microneedles, mucoadhesive patches, and various microdevices present unique drug-carrying capabilities. The current work presents a novel soft stent platform that can facilitate contact between the small intestine tissue and drug carriers to enhance drug absorption and increase residence time. This study aims to prove the concept of this novel platform and determine if the soft stent will retain orally to the ileocecal valve longer than a capsule-shaped bolus. Benchtop studies on an intestinal simulator showed successful retention of the soft stent compared to a control capsule. In vivo studies in pig models also showed that the soft stent was retained longer than the control capsule. Overall, this study shows promise that this novel platform could be used for oral drug delivery of biologics.

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 Efficient Treatment of Fish Intestinal Parasites Applying Biocompatible Membrane-penetrating Oral Drug Delivery Nanoparticles

2021 ◽  
Author(s):  
Patrick D. Mathews ◽  
Ana C.M.F. Patta ◽  
Rafael R.M. Madrid ◽  
Carlos A.B. Ramirez ◽  
Omar Mertins
Keyword(s):  
Drug Delivery ◽  
Oral Drug Delivery ◽  
Intestinal Parasites ◽  
Drug Stability ◽  
Pharmacological Action ◽  
Oral Route ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Efficient Treatment

Abstract Nanodelivery of drugs aims to ensure drug stability in the face of adverse biochemical conditions in the course of administration, concomitant with appropriate pharmacological action provided by delivery at the targeted site. In this study, the application potential of nanoparticles produced with biopolymers chitosan-N-arginine and alginate as an oral drug delivery material is evaluated. Being both macromolecules weak polyelectrolytes, the bioparticle presents strong thermodynamic interaction with a biological model membrane consisting of charged lipid liposome bilayer, leading to membrane disruption and membrane penetration of the bioparticles in ideal conditions of pH corresponding to the oral route. The powder form of the bioparticle was obtained by lyophilization and with a high percentage of entrapment of the anthelmintic drug praziquantel. In vivo studies were conducted with oral administration to Corydoras schwartzi fish with high intensity of intestinal parasites infection. The in vivo experiments confirmed the mucoadhesive and revealed membrane-penetrating properties of the bioparticle by translocating the parasite cyst, which provided target drug release and reduction of over 97% of the fish intestinal parasites. Thus, it was evidenced that the bioparticle was effective in transporting and releasing the drug to the target, providing an efficient treatment.

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.

REVIEW ON GASTRORETENTIVE DRUG DELIVERY SYSTEM

2020 ◽  
pp. 38-45
Author(s):  
MANDAR J BHANDWALKAR ◽  
PRASAD S DUBAL ◽  
AKASH K.TUPE ◽  
SUPRIYA N MANDRUPKAR
Keyword(s):  
Drug Delivery ◽  
Small Intestine ◽  
Drug Delivery System ◽  
Residence Time ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Dosage Forms ◽  
Oral Dosage ◽  
Oral Drug ◽  
Low Solubility

In recent years, gastroretentive drug delivery system (GRDDS) has gained researcher’s interest in the field of oral drug delivery. Various GRDDS approaches can be utilized to retain the dosage forms in the stomach and to release the drug slowly for an extended period of time. GRDDS can be used to prolong the residence time of delivery system in the stomach. This results in targeting of drug release at a specific site for the systemic or local effects. GRDDS can be used to overcome challenges associated with conventional oral dosage forms and to release the drug at a specific absorption site to improve bioavailability of particular drug substance. The challenges include fast gastric emptying of the dosage form which results in the poor bioavailability of the drug. Prolongation of the retention of drugs in stomach those having low solubility at high intestinal pH improves the solubility of drugs. GRDDS has proved to be effective in systemic actions as well as in local actions to treat gastric or duodenal ulcers. Local activity in the upper part of the small intestine can be obtained by improving the residence time of delivery system in the stomach. The system is useful for drugs which are unstable in the intestine or having a low solubility/permeability in the small intestine. Various GRDDS approaches include high density (sinking) systems, low-density (floating systems), mucoadhesive, expandable, unfoldable, superporous hydrogel systems, and magnetic systems.

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

Evaluation of mesoporous silica nanoparticles for oral drug delivery – current status and perspective of MSNs drug carriers

Nanoscale ◽  
2017 ◽  
Vol 9 (40) ◽  
pp. 15252-15277 ◽  
Author(s):  
Justyna Florek ◽  
Romain Caillard ◽  
Freddy Kleitz
Keyword(s):  
Drug Delivery ◽  
Mesoporous Silica ◽  
Drug Delivery Systems ◽  
Oral Drug Delivery ◽  
Mesoporous Silica Nanoparticles ◽  
Drug Carriers ◽  
Current Status ◽  
Oral Drug ◽  
Future Perspectives ◽  
Oral Drug Delivery Systems

Mesoporous silica nanocarriers are discussed as potential oral drug delivery systems, focusing on their advantages and limitations, and future perspectives.

Design, Optimization and Evaluation of Lurasidone Hydrochloride Nanocrystals as Fast Disintegrating Tablets

2019 ◽  
Vol 4 (2) ◽  
pp. 121-129
Author(s):  
Satya Sankar Sahoo ◽  
Chandu Babu Rao
Keyword(s):  
Patient Compliance ◽  
Oral Drug Delivery ◽  
Particle Diameter ◽  
Water Soluble ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Water Soluble Drugs ◽  
Fast Disintegrating Tablets ◽  
Lurasidone Hydrochloride

Formulation of poorly water-soluble drugs for oral drug delivery has always been a difficult task for formulation scientists. Lurasidone hydrochloride is one such agent which is used to control bipolar depre-ssion. The objective of this study was to formulate and optimize lurasi-done nanosuspension, further formulating optimized nanosuspensions as fast disintegrating tablets for improved patient compliance. In the present study, lurasidone nanosuspension was prepared by nanomilling technique. Optimized nanosuspension has mean particle diameter of 248.9 nm, polydispersity index of 0.127 and zeta potential of 18.1 mV. The lyophilized optimized nanocrystals, optimize nanosuspension as granulating fluid and as top spraying dispersion for granulation in fluid bed granulator being used to formulate fast disintegrating tablets with suitable super disintegrant. Croscarmellose sodium was found to be best superdisintegrant compared to sodium starch glycolate and crospovidone, as its acts by both mechanism swelling and wicking. Its swells 4-8 folds in less than 10 s. Many folds increase in the rate of drug release observed compare to micronized lurasidone and marketed product. There was no change in crystalline nature after nanomilling as characterized by XRD and FTIR, and it was found to be chemically stable with high drug content. The developed fast disintegrating tablets would be an alternative better formulation than its conventional formulation to address its bioavailability issue and for improved patient compliance. However, this should be further confirmed by appropriate in vivo studies.

scholarly journals A Critical Appraisal of Solubility Enhancement Techniques of Polyphenols

2014 ◽  
Vol 2014 ◽  
pp. 1-14 ◽  
Author(s):  
Harkiran Kaur ◽  
Gurpreet Kaur
Keyword(s):  
Drug Delivery ◽  
Critical Appraisal ◽  
Oral Drug Delivery ◽  
Aqueous Solubility ◽  
Solubility Enhancement ◽  
Oral Drug ◽  
Natural Substances ◽  
First Pass ◽  
Cellular Dna

Polyphenols constitute a family of natural substances distributed widely in plant kingdom. These are produced as secondary metabolites by plants and so far 8000 representatives of this family have been identified. Recently, there is an increased interest in the polyphenols because of the evidence of their role in prevention of degenerative diseases such as neurodegenerative diseases, cancer, and cardiovascular diseases. Although a large number of drugs are available in the market for treatment of these diseases, however, the emphasis these days is on the exploitation of natural principles derived from plants. Most polyphenols show low in vivo bioavailability thus limiting their application for oral drug delivery. This low bioavailability could be associated with low aqueous solubility, first pass effect, metabolism in GIT, or irreversible binding to cellular DNA and proteins. Therefore, there is a need to devise strategies to improve oral bioavailability of polyphenols. Various approaches like nanosizing, self-microemulsifying drug delivery systems (SMEDDS), microencapsulation, complexation, and solid dispersion can be used to increase the bioavailability. This paper will highlight the various methods that have been employed till date for the solubility enhancement of various polyphenols so that a suitable drug delivery system can be formulated.

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