Vancomycin and insulin used as models for oral delivery of peptides

Geary, Richard S.; Schlameus, H. Wade

doi:10.1016/0168-3659(93)90071-c

Cited by 36 publications

(7 citation statements)

References 18 publications

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“…It was reported that infection by MRSA was cured with this method without serious nephrotoxicity. In a previous study, we reported on the use of a w/o/w emulsion for sustained release of VCM (Geary and Schlameus 1993;Okochi and Nakano 1996b). Thus, the emulsion may be considered useful for maintaining VCM serum concentration after intravenous administration.…”

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confidence: 96%

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Pharmacokinetics of Vancomycin after Intravenous Administration of a W/O/W Emulsion to Rats

Okochi

Nakano

1997

Drug Delivery

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A stable water-in-oil-in-water multiple emulsion (wIo/w emulsion) was prepared, and its potential for drug delivery was evaluated. Wlolw emulsions were prepared using a Lipiodol Ultra-Fluid@ and isopropyl myristate oil mixture for the oily phase and vancomycin (VCM) for the entrapped drug. The surfactants, HCO-40 (5% [w/v]) and Pluronic F-88 were dissolved in the oily phase and the external aqueous phase, respectively. Resultant w/o/w emulsions were evaluated for entrapment efficiency, particle size, viscosity, drug release in vitro, and disposition kinetics of the drug and the wlolw emulsion in vivo. The particle size of the w/o/w emulsion decreased with an increase in the concentration of F-88 in the external aqueous phase and stirring speed at the second emulsification stage (the smallest being 2.9 f 1.5 pm). Entrapment efficiency of VCM in the wlolw emulsion decreased with an increase in the concentration of F-88 (the maximum being 65.3 f 5.4%). VCM release from the wlolw emulsion was prolonged and tended to be slower with an increase in the particle size of the emulsion. After intravenous administration, significant differences in pharmacokinetic parameters, such as kzl, kelp, AUCO-,, MRTM, and MRTo-,, were observed between the VCM solution and the wlolw emulsion-entrapped drug. When the wlolw emulsion with Sudan I1 in the oily phase was administered intravenously, the emulsion accumulated in the lung at first (the highest value was observed just after administration) and then in the liver (the highest value was observed at 60 min). The wlolw emulsion prepared in this study is expected to be a possible carrier for the prolonged release of water-soluble drugs after intravenous administration.

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confidence: 96%

“…Because VCM is a glycopeptide antibiotic and has six peptide bonds in its structure, the drug has been used as a model of a peptide drug entrapped in microspheres (Geary and Schlameus 1993). VCM is used for the treatment of infections caused by methicillin-resistant Staphylococcus uureus (MRSA).…”

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confidence: 99%

Pharmacokinetics of Vancomycin after Intravenous Administration of a W/O/W Emulsion to Rats

Okochi

Nakano

1997

Drug Delivery

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“…10 There are very few investigations reported for improving the GI absorption of Vancomycin hydrochloride by using strategies such as 12 and using sodium glycocholate as absorption promoter. 13 Liposomes, the colloidal vesicular structures due to their biphasic environment can act as carriers for both lipophilic & hydrophilic drugs. High hydrophilic drug (log p<-0.3) are located exclusively in the aqueous domains, whereas highly lipophilic drugs (log P>5) are entrapped within the lipid bilayers of the liposomes.…”

Section: Introductionmentioning

confidence: 99%

Design and Development of Vancomycin Liposomes

Srinivas¹,

Tenneti²,

Nimmali³

2015

IJPER

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Vancomycin hydrochloride is water soluble and poorly absorbable glycopeptide antibiotic act by inhibition of the synthesis of peptidoglycan a major component of bacteria cell wall. It is highly effective against the Staphylococcus aureus and other Staphylococcus species microorganisms. Structurally vancomycin hydrochloride has six peptide bonds with a molecular weight of approximately 1500 Da. Liposomes, the colloidal vesicular structures due to their biphasic environment can act as carriers for both lipophilic & hydrophilic drugs. The encapsulation of antimicrobials in liposomes potentially offers enhanced pharmacokinetics and pharmacodynamics and decreased toxicity. This delivery system has the advantages of targeted, long circulation, low toxicity, sustained-release, no immunogenicity and protecting the encapsulated drugs from the destructive action of the external media. The present research work is planned to develop liposomal formulation of Vancomycin hydrochloride and to study the possibility of permeability enhancement. Liposomes are prepared by using various permeation enhancers like propylene glycol, poly ethylene glycol 400, poly ethylene glycol 600, Tween 80 and Span 60. The prepared liposomes are characterized by optical microscopy, scanning electron microscopy, particle size determination, encapsulation efficiency, FTIR spectroscopy studies and in vitro diffusion studies using dialysis membrane. Among six different liposomes F2 formulation (containing propylene glycol) has showed promising results with respect to drug entrapment and percentage drug release.

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“…Bioadhesive microspheres Buccal, oral, ocular, nasal, colonic drug delivery Nasal -Gentamicin, Insulin (19) , GI -Glipizide (20) Colonic -Insulin (21) , Ocular -Methyl prednisolone (22) Magnetic microspheres Used in DNA analysis, cell isolation, protein purification and targetting drugs to tumour sites( Doxorubicin) (4) (7) Floating microspheres Carriers for drugs like antiviral, antifungal and antibiotic agents(so called absorption windows), non-steroidal anti inflammatory drugs, Prednisolone, Lansoprazole (4)(8) (23) Radioactive microspheres For diagnostic purpose -Diagnostic radioembolization: 99m Tc-macroaggregated human serum albumin (MAA) (24) , Thrombus imaging in deep vein thrombosis : 99 mTc-sulfur colloid (25) For therapeutic purpose -Radioembolization of liver and spleen tumours: 90 Ymicrospheres (26) , Local radiotherapy: 212 Pb-sulfur colloid (26) .…”

Section: Applications (3) (4) : Type Of Microspheres Applicationsmentioning

confidence: 99%

Microspheres: as carrieres used for novel drug delivery system

H¹,

B²,

Dhole³

2012

iosrphr

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The goal of any drug delivery system is to provide a therapeutic amount of drug to the proper site in the body and then maintain the desired drug concentration. A well designed controlled drug delivery system can overcome some of problems of conventional therapy and enhance therapeutic efficacy of the given drug. There are various approaches in delivering therapeutic substance to the target site in sustained and controlled release fashion. One such approach is using microspheres as carriers for drug. Microspheres are characteristically free flowing powders consisting of proteins or synthetic polymers which are biodegradable in nature ideally having particle size less than 200μm.Various synthetic and natural materials are used for the preparation of microspheres. These are prepared by methods like Single emulsion, Double emulsion, Polymerization, Phase separation coacervation, Emulsion solvent evaporation and solvent diffusion. Microspheres are having wide range of applications because of controlled and sustained release. Most important application is that it is used for targeting tumours using anticancer drugs. It is important carrier for safe and effective in vivo drug delivery.

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Vancomycin and insulin used as models for oral delivery of peptides

Cited by 36 publications

References 18 publications

Pharmacokinetics of Vancomycin after Intravenous Administration of a W/O/W Emulsion to Rats

Pharmacokinetics of Vancomycin after Intravenous Administration of a W/O/W Emulsion to Rats

Design and Development of Vancomycin Liposomes

Microspheres: as carrieres used for novel drug delivery system

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