Formulation and evaluation of mucoadhesive glipizide films

Glipizide is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach f...

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Veröffentlicht in:Acta pharmaceutica (Zagreb, Croatia) Croatia), 2011-06, Vol.61 (2), p.203-216
Hauptverfasser: Rajput, Ganesh, Majmudar, Falguni, Patel, Jayvadan
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Patel, Jayvadan
description Glipizide is mainly absorbed in the proximal areas of the gastrointestinal tract. The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect. Glipizid se pretežno apsorbira u proksimalnom dijelu gastrointestinalnog trakta. Cilj rada je priprava i evaluacija mukoadhezivnih filmova s kojima bi se produljilo zadržavanje lijeka u predjelu apsorpcije. Pripravljeni su mukoadhezivni filmovi glipizida koji se produljeno zadržavaju u želucu. Polimerni filmovi sadržavali su različite količine hidroksipropil celuloze i polietilen glikola 400 (PEG 400). Evaluirana su sljedeća svojstva mukoadhezivnih filmova: čvrstoća, postotak elongacije, indeks bubrenja, sadržaj vlage, pH i viskoznost polimerne disperzije, debljina filma, koncentracija lijeka, jednolikost i mukoadhezivnost u simuliranom želučanom soku. Na dinamičkom modelu želuca određ ivan je i postotak lijeka koji se zadržava u sluznici želuca u ovisnosti o vremenu. Poveć anjem koncentracije hidroksipropil celuloze povećavaju se čvrstoća i elongacija, dok se povećanje koncentracije PEG 400 reflektira na smanjenje čvrstoće i povećanje elongacije kod loma. Omjer glipizid/hidroksipropil celuloza/PEG 400 (2,5:1:0,5)
doi_str_mv 10.2478/v10007-011-0017-3
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The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect. Glipizid se pretežno apsorbira u proksimalnom dijelu gastrointestinalnog trakta. Cilj rada je priprava i evaluacija mukoadhezivnih filmova s kojima bi se produljilo zadržavanje lijeka u predjelu apsorpcije. Pripravljeni su mukoadhezivni filmovi glipizida koji se produljeno zadržavaju u želucu. Polimerni filmovi sadržavali su različite količine hidroksipropil celuloze i polietilen glikola 400 (PEG 400). Evaluirana su sljedeća svojstva mukoadhezivnih filmova: čvrstoća, postotak elongacije, indeks bubrenja, sadržaj vlage, pH i viskoznost polimerne disperzije, debljina filma, koncentracija lijeka, jednolikost i mukoadhezivnost u simuliranom želučanom soku. Na dinamičkom modelu želuca određ ivan je i postotak lijeka koji se zadržava u sluznici želuca u ovisnosti o vremenu. Poveć anjem koncentracije hidroksipropil celuloze povećavaju se čvrstoća i elongacija, dok se povećanje koncentracije PEG 400 reflektira na smanjenje čvrstoće i povećanje elongacije kod loma. Omjer glipizid/hidroksipropil celuloza/PEG 400 (2,5:1:0,5) (GF5) bio je optimalan za pripravu mukoadhezivnih formulacija, s dobrom kalavošću, relativno visokim indeksom bubrenja, umjerenom čvrstoćom te zadržavanjem u sluznici želuca štakora do 8 h. 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The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. 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Polimerni filmovi sadržavali su različite količine hidroksipropil celuloze i polietilen glikola 400 (PEG 400). Evaluirana su sljedeća svojstva mukoadhezivnih filmova: čvrstoća, postotak elongacije, indeks bubrenja, sadržaj vlage, pH i viskoznost polimerne disperzije, debljina filma, koncentracija lijeka, jednolikost i mukoadhezivnost u simuliranom želučanom soku. Na dinamičkom modelu želuca određ ivan je i postotak lijeka koji se zadržava u sluznici želuca u ovisnosti o vremenu. Poveć anjem koncentracije hidroksipropil celuloze povećavaju se čvrstoća i elongacija, dok se povećanje koncentracije PEG 400 reflektira na smanjenje čvrstoće i povećanje elongacije kod loma. Omjer glipizid/hidroksipropil celuloza/PEG 400 (2,5:1:0,5) (GF5) bio je optimalan za pripravu mukoadhezivnih formulacija, s dobrom kalavošću, relativno visokim indeksom bubrenja, umjerenom čvrstoćom te zadržavanjem u sluznici želuca štakora do 8 h. U in vivo testiranjima mukoadhesivni filmovi s glipizidom pokazali su potencijalni hipoglikemijski učinak.</description><subject>Adhesiveness</subject><subject>Animals</subject><subject>Blood Glucose - analysis</subject><subject>Cellulose - analogs &amp; derivatives</subject><subject>Cellulose - chemistry</subject><subject>Chemical Phenomena</subject><subject>Delayed-Action Preparations</subject><subject>desirability function</subject><subject>Drug Carriers - administration &amp; dosage</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Carriers - pharmacology</subject><subject>Drug Compounding</subject><subject>Excipients - chemistry</subject><subject>factorial design</subject><subject>faktorijalno dizajniranje</subject><subject>Female</subject><subject>funkcija poželjnosti</subject><subject>Gastric Mucosa - metabolism</subject><subject>glipizid</subject><subject>glipizide</subject><subject>Glipizide - administration &amp; dosage</subject><subject>Glipizide - chemistry</subject><subject>Glipizide - pharmacology</subject><subject>hipoglikemijski učinak</subject><subject>Hydrogen-Ion Concentration</subject><subject>Hypoglycemic Agents - administration &amp; dosage</subject><subject>Hypoglycemic Agents - chemistry</subject><subject>Hypoglycemic Agents - pharmacology</subject><subject>hypoglycemic effect</subject><subject>In Vitro Techniques</subject><subject>Male</subject><subject>Mechanical Phenomena</subject><subject>mucoadhesive film</subject><subject>mukoadhezivni film</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Polymers - chemistry</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Specific Pathogen-Free Organisms</subject><subject>Water - analysis</subject><issn>1330-0075</issn><issn>1846-9558</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNpdkE1LxDAQhoMofv8AL1Lw4Kk6-U68-a2wIsIqewuxnWq03a7NdlF_vZGqBy9JhnnmZfIQskPhgAltDhcUAHQOlOYAVOd8iaxTI1RupTTL6c05pI6Wa2QjxhcAobVhq2SNUWWEEXqdHF20XdPXfh7aaeanZYYLX_dD2VZZ0xetL58xhgVmT3WYhc9QYlaFuolbZKXydcTtn3uT3F-cj0-v8tHt5fXp8SgvBNh5LkvLFDKOVUFLo4WmUmmPYDUa-QiYPqKstIIbqpSpqrRvYRgz6VBSCuSbZH_InXXtW49x7poQC6xrP8W2j85YI0EzBonc-0e-tH03Tcs5yqlNqWBpouhAFV0bY4eVm3Wh8d2Ho-C-vbrBq0te3bdXx9PM7k9y_9hg-TfxKzIB-QCEOMf3v77vXp3SXEt3NxZO30wmI_tw5k74F3b5f-U</recordid><startdate>20110601</startdate><enddate>20110601</enddate><creator>Rajput, Ganesh</creator><creator>Majmudar, Falguni</creator><creator>Patel, Jayvadan</creator><general>Versita</general><general>De Gruyter Poland</general><scope>BSCLL</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>BYOGL</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>7X8</scope></search><sort><creationdate>20110601</creationdate><title>Formulation and evaluation of mucoadhesive glipizide films</title><author>Rajput, Ganesh ; Majmudar, Falguni ; Patel, Jayvadan</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c409t-5d926e23efc1d87471567ae097e85b0e47869594381668ff007c8228c826554e3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Adhesiveness</topic><topic>Animals</topic><topic>Blood Glucose - analysis</topic><topic>Cellulose - analogs &amp; derivatives</topic><topic>Cellulose - chemistry</topic><topic>Chemical Phenomena</topic><topic>Delayed-Action Preparations</topic><topic>desirability function</topic><topic>Drug Carriers - administration &amp; dosage</topic><topic>Drug Carriers - chemistry</topic><topic>Drug Carriers - pharmacology</topic><topic>Drug Compounding</topic><topic>Excipients - chemistry</topic><topic>factorial design</topic><topic>faktorijalno dizajniranje</topic><topic>Female</topic><topic>funkcija poželjnosti</topic><topic>Gastric Mucosa - metabolism</topic><topic>glipizid</topic><topic>glipizide</topic><topic>Glipizide - administration &amp; dosage</topic><topic>Glipizide - chemistry</topic><topic>Glipizide - pharmacology</topic><topic>hipoglikemijski učinak</topic><topic>Hydrogen-Ion Concentration</topic><topic>Hypoglycemic Agents - administration &amp; dosage</topic><topic>Hypoglycemic Agents - chemistry</topic><topic>Hypoglycemic Agents - pharmacology</topic><topic>hypoglycemic effect</topic><topic>In Vitro Techniques</topic><topic>Male</topic><topic>Mechanical Phenomena</topic><topic>mucoadhesive film</topic><topic>mukoadhezivni film</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Polymers - chemistry</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Specific Pathogen-Free Organisms</topic><topic>Water - analysis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Rajput, Ganesh</creatorcontrib><creatorcontrib>Majmudar, Falguni</creatorcontrib><creatorcontrib>Patel, Jayvadan</creatorcontrib><collection>Istex</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Health &amp; 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The purpose of this study was formulation and evaluation of mucoadhesive films to prolong the stay of drug in its absorption area. Glipizide was formulated in a mucoadhesive film that could be retained in the stomach for prolonged intervals. Polymeric films were designed with various compositions of hydroxypropyl cellulose and polyethylene glycol 400 (PEG 400). Properties of the mucoadhesive film such as tensile strength, percentage elongation, swelling index, moisture content, pH and viscosity of polymeric dispersion, film thickness, content uniformity and mucoadhesion in a simulated gastric environment were characterized. In addition, percentage drug retained in stomach mucosa was estimated using a simulated dynamic stomach system as a function of time. Increase in hydroxypropyl cellulose concentration resulted in a higher tensile strength and elongation at break, while increase in concentration of PEG 400 was reflected in a decrease in tensile strength and increase of elongation at break. Glipizide/hydroxypropyl cellulose/PEG 400 (2.5:1:0.5) (GF5) was found to be the optimal composition for a novel mucoadhesive stomach formulation that showed good peelability, relatively high swelling index, moderate tensile strength, and stayed on rat stomach mucosa up to 8 h. In vivo testing of the mucoadhesive films with glipizide demonstrated a potential hypoglycemic effect. Glipizid se pretežno apsorbira u proksimalnom dijelu gastrointestinalnog trakta. Cilj rada je priprava i evaluacija mukoadhezivnih filmova s kojima bi se produljilo zadržavanje lijeka u predjelu apsorpcije. Pripravljeni su mukoadhezivni filmovi glipizida koji se produljeno zadržavaju u želucu. Polimerni filmovi sadržavali su različite količine hidroksipropil celuloze i polietilen glikola 400 (PEG 400). Evaluirana su sljedeća svojstva mukoadhezivnih filmova: čvrstoća, postotak elongacije, indeks bubrenja, sadržaj vlage, pH i viskoznost polimerne disperzije, debljina filma, koncentracija lijeka, jednolikost i mukoadhezivnost u simuliranom želučanom soku. Na dinamičkom modelu želuca određ ivan je i postotak lijeka koji se zadržava u sluznici želuca u ovisnosti o vremenu. Poveć anjem koncentracije hidroksipropil celuloze povećavaju se čvrstoća i elongacija, dok se povećanje koncentracije PEG 400 reflektira na smanjenje čvrstoće i povećanje elongacije kod loma. Omjer glipizid/hidroksipropil celuloza/PEG 400 (2,5:1:0,5) (GF5) bio je optimalan za pripravu mukoadhezivnih formulacija, s dobrom kalavošću, relativno visokim indeksom bubrenja, umjerenom čvrstoćom te zadržavanjem u sluznici želuca štakora do 8 h. U in vivo testiranjima mukoadhesivni filmovi s glipizidom pokazali su potencijalni hipoglikemijski učinak.</abstract><cop>Croatia</cop><pub>Versita</pub><pmid>21684847</pmid><doi>10.2478/v10007-011-0017-3</doi><tpages>14</tpages><oa>free_for_read</oa></addata></record>
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source MEDLINE; De Gruyter Open Access Journals; DOAJ Directory of Open Access Journals; EZB-FREE-00999 freely available EZB journals
subjects Adhesiveness
Animals
Blood Glucose - analysis
Cellulose - analogs & derivatives
Cellulose - chemistry
Chemical Phenomena
Delayed-Action Preparations
desirability function
Drug Carriers - administration & dosage
Drug Carriers - chemistry
Drug Carriers - pharmacology
Drug Compounding
Excipients - chemistry
factorial design
faktorijalno dizajniranje
Female
funkcija poželjnosti
Gastric Mucosa - metabolism
glipizid
glipizide
Glipizide - administration & dosage
Glipizide - chemistry
Glipizide - pharmacology
hipoglikemijski učinak
Hydrogen-Ion Concentration
Hypoglycemic Agents - administration & dosage
Hypoglycemic Agents - chemistry
Hypoglycemic Agents - pharmacology
hypoglycemic effect
In Vitro Techniques
Male
Mechanical Phenomena
mucoadhesive film
mukoadhezivni film
Polyethylene Glycols - chemistry
Polymers - chemistry
Rats
Rats, Wistar
Specific Pathogen-Free Organisms
Water - analysis
title Formulation and evaluation of mucoadhesive glipizide films
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