Controlled release polymeric ocular delivery of acyclovir
The aim of the present study was to formulate and evaluate controlled release polymeric ocular delivery of acyclovir. Reservoir-type ocular inserts were fabricated by sandwiching hydroxypropyl methylcellulose (HPMC) matrix film containing acyclovir between two rate controlling membranes of cellulose...
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| Veröffentlicht in: | Pharmaceutical development and technology 2010-08, Vol.15 (4), p.369-378 |
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| container_title | Pharmaceutical development and technology |
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| creator | Deshpande, Praful Balavant Dandagi, Panchaxari Udupa, Nayanabhirama Gopal, Shavi V. Jain, Samata S. Vasanth, Surenalli G. |
| description | The aim of the present study was to formulate and evaluate controlled release polymeric ocular delivery of acyclovir. Reservoir-type ocular inserts were fabricated by sandwiching hydroxypropyl methylcellulose (HPMC) matrix film containing acyclovir between two rate controlling membranes of cellulose acetate phthalate (CAP). The solubility and dissolution rate of poorly soluble acyclovir was enhanced by preparing binary systems with β-cyclodextrin and then incorporated into HPMC matrix. Nine formulations (AB-1 to AB-9) with varying ratio of HPMC (drug matrix) and CAP (rate controlling membrane) were developed and sterilized by gamma radiation. The formulations were subjected to various physico-chemical evaluations. The in vitro release profile of all the formulations showed a steady, controlled drug release up to 20 h with non-Fickian diffusion behavior. A high correlation coefficient found between in vitro/in vivo release rate studies. Formation of acyclovir complex was confirmed by differential scanning calorimetry. In addition, dissolution rate studies revealed improved solubility of acyclovir when complexed with β-cyclodextrin. Stability studies showed that the ocular inserts could be stored safely at study storage conditions. In conclusion, the present study demonstrated controlled release formulation of acyclovir inserts for ocular delivery using biodegradable polymers. |
| doi_str_mv | 10.3109/10837450903262017 |
| format | Article |
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Reservoir-type ocular inserts were fabricated by sandwiching hydroxypropyl methylcellulose (HPMC) matrix film containing acyclovir between two rate controlling membranes of cellulose acetate phthalate (CAP). The solubility and dissolution rate of poorly soluble acyclovir was enhanced by preparing binary systems with β-cyclodextrin and then incorporated into HPMC matrix. Nine formulations (AB-1 to AB-9) with varying ratio of HPMC (drug matrix) and CAP (rate controlling membrane) were developed and sterilized by gamma radiation. The formulations were subjected to various physico-chemical evaluations. The in vitro release profile of all the formulations showed a steady, controlled drug release up to 20 h with non-Fickian diffusion behavior. A high correlation coefficient found between in vitro/in vivo release rate studies. Formation of acyclovir complex was confirmed by differential scanning calorimetry. In addition, dissolution rate studies revealed improved solubility of acyclovir when complexed with β-cyclodextrin. Stability studies showed that the ocular inserts could be stored safely at study storage conditions. In conclusion, the present study demonstrated controlled release formulation of acyclovir inserts for ocular delivery using biodegradable polymers.</description><identifier>ISSN: 1083-7450</identifier><identifier>EISSN: 1097-9867</identifier><identifier>DOI: 10.3109/10837450903262017</identifier><identifier>PMID: 19772377</identifier><language>eng</language><publisher>England: Informa UK Ltd</publisher><subject>Acyclovir ; Acyclovir - administration & dosage ; Acyclovir - chemistry ; Administration, Topical ; Animals ; Antiviral Agents - administration & dosage ; Antiviral Agents - chemistry ; beta-Cyclodextrins - chemistry ; binary systems ; Cellulose - analogs & derivatives ; Cellulose - chemistry ; Delayed-Action Preparations ; differential scanning calorimetry ; Diffusion ; Drug Carriers - chemistry ; Drug Delivery Systems ; Drug Stability ; Drug Storage ; Gamma Rays ; Hypromellose Derivatives ; Male ; Methylcellulose - analogs & derivatives ; Methylcellulose - chemistry ; ocular insert ; Polymers - chemistry ; Rabbits ; Solubility ; Time Factors ; β-cyclodextrin</subject><ispartof>Pharmaceutical development and technology, 2010-08, Vol.15 (4), p.369-378</ispartof><rights>2010 Informa UK Ltd 2010</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c320t-7b2b5d60401d49266d6805e32f9ea7cbc79d140fb0e67cb023064291e10dafcc3</citedby><cites>FETCH-LOGICAL-c320t-7b2b5d60401d49266d6805e32f9ea7cbc79d140fb0e67cb023064291e10dafcc3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>315,781,785,27929,27930</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19772377$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Deshpande, Praful Balavant</creatorcontrib><creatorcontrib>Dandagi, Panchaxari</creatorcontrib><creatorcontrib>Udupa, Nayanabhirama</creatorcontrib><creatorcontrib>Gopal, Shavi V.</creatorcontrib><creatorcontrib>Jain, Samata S.</creatorcontrib><creatorcontrib>Vasanth, Surenalli G.</creatorcontrib><title>Controlled release polymeric ocular delivery of acyclovir</title><title>Pharmaceutical development and technology</title><addtitle>Pharm Dev Technol</addtitle><description>The aim of the present study was to formulate and evaluate controlled release polymeric ocular delivery of acyclovir. Reservoir-type ocular inserts were fabricated by sandwiching hydroxypropyl methylcellulose (HPMC) matrix film containing acyclovir between two rate controlling membranes of cellulose acetate phthalate (CAP). The solubility and dissolution rate of poorly soluble acyclovir was enhanced by preparing binary systems with β-cyclodextrin and then incorporated into HPMC matrix. Nine formulations (AB-1 to AB-9) with varying ratio of HPMC (drug matrix) and CAP (rate controlling membrane) were developed and sterilized by gamma radiation. The formulations were subjected to various physico-chemical evaluations. The in vitro release profile of all the formulations showed a steady, controlled drug release up to 20 h with non-Fickian diffusion behavior. A high correlation coefficient found between in vitro/in vivo release rate studies. Formation of acyclovir complex was confirmed by differential scanning calorimetry. In addition, dissolution rate studies revealed improved solubility of acyclovir when complexed with β-cyclodextrin. Stability studies showed that the ocular inserts could be stored safely at study storage conditions. In conclusion, the present study demonstrated controlled release formulation of acyclovir inserts for ocular delivery using biodegradable polymers.</description><subject>Acyclovir</subject><subject>Acyclovir - administration & dosage</subject><subject>Acyclovir - chemistry</subject><subject>Administration, Topical</subject><subject>Animals</subject><subject>Antiviral Agents - administration & dosage</subject><subject>Antiviral Agents - chemistry</subject><subject>beta-Cyclodextrins - chemistry</subject><subject>binary systems</subject><subject>Cellulose - analogs & derivatives</subject><subject>Cellulose - chemistry</subject><subject>Delayed-Action Preparations</subject><subject>differential scanning calorimetry</subject><subject>Diffusion</subject><subject>Drug Carriers - chemistry</subject><subject>Drug Delivery Systems</subject><subject>Drug Stability</subject><subject>Drug Storage</subject><subject>Gamma Rays</subject><subject>Hypromellose Derivatives</subject><subject>Male</subject><subject>Methylcellulose - analogs & derivatives</subject><subject>Methylcellulose - chemistry</subject><subject>ocular insert</subject><subject>Polymers - chemistry</subject><subject>Rabbits</subject><subject>Solubility</subject><subject>Time Factors</subject><subject>β-cyclodextrin</subject><issn>1083-7450</issn><issn>1097-9867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1LxDAQhoMofv8AL9Kbp-okaZsGvcjiFwhe9FzSZIqVtFknrdJ_b5ddEBE9TSY878PwMnbC4Vxy0BccSqmyHDRIUQjgaovtz_8q1WWhtlfvUqYrYI8dxPgGwEsN-S7b41opIZXaZ3oR-oGC9-gSQo8mYrIMfuqQWpsEO3pDiUPffiBNSWgSYyfrw0dLR2ynMT7i8WYespfbm-fFffr4dPewuH5MrRQwpKoWde4KyIC7TIuicEUJOUrRaDTK1lZpxzNoasBiXkFIKDKhOXJwprFWHrKztXdJ4X3EOFRdGy16b3oMY6yUlDlkQmYzydekpRAjYVMtqe0MTRWHalVY9auwOXO6sY91h-47sWloBq7WQNs3gTrzGci7ajCTD9SQ6W0bV-6__Zc_4q9o_PBqDWH1Fkbq5-b-ue4LvGyKmA</recordid><startdate>20100801</startdate><enddate>20100801</enddate><creator>Deshpande, Praful Balavant</creator><creator>Dandagi, Panchaxari</creator><creator>Udupa, Nayanabhirama</creator><creator>Gopal, Shavi V.</creator><creator>Jain, Samata S.</creator><creator>Vasanth, Surenalli G.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</general><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>7X8</scope></search><sort><creationdate>20100801</creationdate><title>Controlled release polymeric ocular delivery of acyclovir</title><author>Deshpande, Praful Balavant ; 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Reservoir-type ocular inserts were fabricated by sandwiching hydroxypropyl methylcellulose (HPMC) matrix film containing acyclovir between two rate controlling membranes of cellulose acetate phthalate (CAP). The solubility and dissolution rate of poorly soluble acyclovir was enhanced by preparing binary systems with β-cyclodextrin and then incorporated into HPMC matrix. Nine formulations (AB-1 to AB-9) with varying ratio of HPMC (drug matrix) and CAP (rate controlling membrane) were developed and sterilized by gamma radiation. The formulations were subjected to various physico-chemical evaluations. The in vitro release profile of all the formulations showed a steady, controlled drug release up to 20 h with non-Fickian diffusion behavior. A high correlation coefficient found between in vitro/in vivo release rate studies. Formation of acyclovir complex was confirmed by differential scanning calorimetry. In addition, dissolution rate studies revealed improved solubility of acyclovir when complexed with β-cyclodextrin. Stability studies showed that the ocular inserts could be stored safely at study storage conditions. In conclusion, the present study demonstrated controlled release formulation of acyclovir inserts for ocular delivery using biodegradable polymers.</abstract><cop>England</cop><pub>Informa UK Ltd</pub><pmid>19772377</pmid><doi>10.3109/10837450903262017</doi><tpages>10</tpages></addata></record> |
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| source | MEDLINE; EBSCOhost Business Source Complete |
| subjects | Acyclovir Acyclovir - administration & dosage Acyclovir - chemistry Administration, Topical Animals Antiviral Agents - administration & dosage Antiviral Agents - chemistry beta-Cyclodextrins - chemistry binary systems Cellulose - analogs & derivatives Cellulose - chemistry Delayed-Action Preparations differential scanning calorimetry Diffusion Drug Carriers - chemistry Drug Delivery Systems Drug Stability Drug Storage Gamma Rays Hypromellose Derivatives Male Methylcellulose - analogs & derivatives Methylcellulose - chemistry ocular insert Polymers - chemistry Rabbits Solubility Time Factors β-cyclodextrin |
| title | Controlled release polymeric ocular delivery of acyclovir |
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