scholarly journals Enhanced Oral Delivery of Docetaxel Using Thiolated Chitosan Nanoparticles: Preparation, In Vitro and In Vivo Studies

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Shahrooz Saremi ◽  
Rassoul Dinarvand ◽  
Abbas Kebriaeezadeh ◽  
Seyed Nasser Ostad ◽  
Fatemeh Atyabi
Keyword(s):  
Oral Bioavailability ◽  
Oral Drug Delivery ◽  
Drug Loading ◽  
Cell Monolayer ◽  
Chitosan Nanoparticles ◽  
Positive Control ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Thiolated Chitosan

The aim of this study was to evaluate a nanoparticulate system with mucoadhesion properties composed of a core of polymethyl methacrylate surrounded by a shell of thiolated chitosan (Ch-GSH-pMMA) for enhancing oral bioavailability of docetaxel (DTX), an anticancer drug. DTX-loaded nanoparticles were prepared by emulsion polymerization method using cerium ammonium nitrate as an initiator. Physicochemical properties of the nanoparticles such as particle size, size distribution, morphology, drug loading, and entrapment efficiency were characterized. The pharmacokinetic study was carried out in vivo using wistar rats. The half-life of DTX-loaded NPs was about 9 times longer than oral DTX used as positive control. The oral bioavailability of DTX was increased to 68.9% for DTX-loaded nanoparticles compared to 6.5% for positive control. The nanoparticles showed stronger effect on the reduction of the transepithelial electrical resistance (TEER) of Caco-2 cell monolayer by opening the tight junctions. According to apparent permeability coefficient (Papp) results, the DTX-loaded NPs showed more specific permeation across the Caco-2 cell monolayer in comparison to the DTX. In conclusion, the nanoparticles prepared in this study showed promising results for the development of an oral drug delivery system for anticancer drugs.

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

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.

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.

scholarly journals Biomimetic insulin-imprinted polymer nanoparticles as a potential oral drug delivery system

2017 ◽  
Vol 67 (2) ◽  
pp. 149-168 ◽  
Author(s):  
Pijush Kumar Paul ◽  
Alongkot Treetong ◽  
Roongnapa Suedee
Keyword(s):  
Molecularly Imprinted Polymers ◽  
Oral Drug Delivery ◽  
Three Dimensional ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Functional Monomers ◽  
Oral Drug Delivery System ◽  
Nanosized Material ◽  
Glucose Reduction

AbstractIn this study, we investigate molecularly imprinted polymers (MIPs), which form a three-dimensional image of the region at and around the active binding sites of pharmaceutically active insulin or are analogous to b cells bound to insulin. This approach was employed to create a welldefined structure within the nanospace cavities that make up functional monomers by cross-linking. The obtained MIPs exhibited a high adsorption capacity for the target insulin, which showed a significantly higher release of insulin in solution at pH 7.4 than at pH 1.2. In vivo studies on diabetic Wistar rats showed that the fast onset within 2 h is similar to subcutaneous injection with a maximum at 4 h, giving an engaged function responsible for the duration of glucose reduction for up to 24 h. These MIPs, prepared as nanosized material, may open a new horizon for oral insulin delivery.

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.

In vivo evaluation of an oral drug delivery system for peptides based on S-protected thiolated chitosan

2012 ◽  
Vol 160 (3) ◽  
pp. 477-485 ◽  
Author(s):  
Sarah Dünnhaupt ◽  
Jan Barthelmes ◽  
Javed Iqbal ◽  
Glen Perera ◽  
Clemens C. Thurner ◽  
...  
Keyword(s):  
Drug Delivery ◽  
Drug Delivery System ◽  
Delivery System ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
In Vivo Evaluation ◽  
Thiolated Chitosan ◽  
Oral Drug Delivery System

scholarly journals Recent advances in improving oral drug bioavailability by cocrystals

Bioimpacts ◽  
2018 ◽  
Vol 8 (4) ◽  
pp. 305-320 ◽  
Author(s):  
Shahram Emami ◽  
Mohammadreza Siahi-Shadbad ◽  
Khosro Adibkia ◽  
Mohammad Barzegar-Jalali
Keyword(s):  
Membrane Permeability ◽  
Oral Bioavailability ◽  
Water Solubility ◽  
Oral Absorption ◽  
Oral Drug Delivery ◽  
Oral Drug ◽  
Drug Bioavailability ◽  
Recent Advances ◽  
Intestinal Membrane

Introduction: Oral drug delivery is the most favored route of drug administration. However, poor oral bioavailability is one of the leading reasons for insufficient clinical efficacy. Improving oral absorption of drugs with low water solubility and/or low intestinal membrane permeability is an active field of research. Cocrystallization of drugs with appropriate coformers is a promising approach for enhancing oral bioavailability. Methods: In the present review, we have focused on recent advances that have been made in improving oral absorption through cocrystallization. The covered areas include supersaturation and its importance on oral absorption of cocrystals, permeability of cocrystals through membranes, drug-coformer pharmacokinetic (PK) interactions, conducting in vivo-in vitro correlations for cocrystals. Additionally, a discussion has been made on the integration of nanocrystal technology with supramolecular design. Marketed cocrystal products and PK studies in human subjects are also reported. Results: Considering supersaturation and consequent precipitation properties is necessary when evaluating dissolution and bioavailability of cocrystals. Appropriate excipients should be included to control precipitation kinetics and to capture solubility advantage of cocrystals. Beside to solubility, cocrystals may modify membrane permeability of drugs. Therefore, cocrystals can find applications in improving oral bioavailability of poorly permeable drugs. It has been shown that cocrystals may interrupt cellular integrity of cellular monolayers which can raise toxicity concerns. Some of coformers may interact with intestinal absorption of drugs through changing intestinal blood flow, metabolism and inhibiting efflux pumps. Therefore, caution should be taken into account when conducting bioavailability studies. Nanosized cocrystals have shown a high potential towards improving absorption of poorly soluble drugs. Conclusions: Cocrystals have found their way from the proof-of-principle stage to the clinic. Up to now, at least two cocrystal products have gained approval from regulatory bodies. However, there are remaining challenges on safety, predicting in vivo behavior and revealing real potential of cocrystals in the human.

FORMULATION AND EVALUATION OF MICROSPHERES FOR NASAL DELIVERY OF ANTI-HYPERTENSIVE DRUG

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (10) ◽  
pp. 21-26
Author(s):  
S. S Shelake ◽  
◽  
R. M Mhetre ◽  
S. V Patil ◽  
S. S Patil ◽  
...  
Keyword(s):  
Drug Release ◽  
Ex Vivo ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Nasal Delivery ◽  
In Vivo Studies ◽  
Oral Drug ◽  
Hypertensive Drug

Lisinopril is used in the treatment of hypertension and heart failure in myocardial infarction and also in diabetic nephropathy. It is very poorly absorbed from GIT. Intranasal administration is an ideal alternative to the parenteral route for systemic drug delivery. Formulating multiparticulate system with mucoadhesive polymers may provide a significant increase in the nasal residence time. The microspheres prepared by emulsion solvent evaporation method were characterized for encapsulation efficiency, drug loading, particle size, surface morphology, degree of swelling, ex vivo mucoadhesion, drug release and ex vivo diffusion studies. Entrapment efficiency of microspheres was in range of 84.95±0.50% to 97.44±0.61% mucoadhesion was 83.76% and 94.41% and drug release up to 40 minutes was 53.66% to 88.32%. In ex vivo studies, the microspheres showed good bioavailability by nasal route compared to oral drug administration. Both in vitro and in vivo studies conclude that combination of Carbopol and HPMC based microspheres are better than single carbopol-based formulation for the delivery of lisinopril.

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.

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