Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation
Objective: To formulate and assess bucco-adhesive films of propranolol hydrochloride for pediatric use. Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and F...
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creator | Mohamad, Soad A. Salem, Hesham Yassin, Heba A. Mansour, Heba F. |
description | Objective: To formulate and assess bucco-adhesive films of propranolol hydrochloride for pediatric use.
Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared films were physically investigated for variation of weight, propranolol content, thickness, surface pH, proportion of moisture, folding endurance and mucoadhesion. In vitro drug release study and kinetic analysis of the corresponding data have been conducted. The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method. The pharmacokinetic parameters of the drug were calculated following administration of the optimized film and the corresponding marketed oral tablets to albino rabbits.
Key Finding: The compatibility study revealed the absence of drug/polymer interaction. The film formulations had suitable mucoadhesive and mechanical properties. The optimized formulation exhibited reasonable drug release that followed Higuchi diffusion pattern. The calculated AUC0-8h presented an enhancement in the bioavailability of propranolol hydrochloride from the selected film formulation by 1.9 times relative to the marketed propranolol oral tablets.
Conclusion: These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery. |
doi_str_mv | 10.2147/DDDT.S267317 |
format | Article |
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Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared films were physically investigated for variation of weight, propranolol content, thickness, surface pH, proportion of moisture, folding endurance and mucoadhesion. In vitro drug release study and kinetic analysis of the corresponding data have been conducted. The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method. The pharmacokinetic parameters of the drug were calculated following administration of the optimized film and the corresponding marketed oral tablets to albino rabbits.
Key Finding: The compatibility study revealed the absence of drug/polymer interaction. The film formulations had suitable mucoadhesive and mechanical properties. The optimized formulation exhibited reasonable drug release that followed Higuchi diffusion pattern. The calculated AUC0-8h presented an enhancement in the bioavailability of propranolol hydrochloride from the selected film formulation by 1.9 times relative to the marketed propranolol oral tablets.
Conclusion: These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery.</description><identifier>ISSN: 1177-8881</identifier><identifier>EISSN: 1177-8881</identifier><identifier>DOI: 10.2147/DDDT.S267317</identifier><identifier>PMID: 33116415</identifier><language>eng</language><publisher>ALBANY: Dove Medical Press Ltd</publisher><subject>Adhesion tests ; Adhesiveness ; Adhesives ; Administration, Buccal ; Adrenergic beta-Antagonists - administration & dosage ; Adrenergic beta-Antagonists - chemistry ; Adrenergic beta-Antagonists - pharmacology ; Animals ; Area Under Curve ; Bioavailability ; Biocompatibility ; Biological Availability ; buccoadhesive ; Calorimetry ; Cheek ; Chemistry, Medicinal ; Child ; Chitosan ; Chromatography, High Pressure Liquid ; Differential scanning calorimetry ; Dosage ; Dosage Forms ; Drug Compounding ; Drug delivery systems ; Drug dosages ; Excipients ; Fourier analysis ; Fourier transforms ; High-performance liquid chromatography ; hplc ; Humans ; Hydrogen-Ion Concentration ; Infant ; Infrared spectroscopy ; Investigations ; Life Sciences & Biomedicine ; Liquid chromatography ; Mathematical analysis ; Mechanical properties ; Moisture content ; Mucin ; Oral administration ; Original Research ; paediatric ; Patient compliance ; Pediatric pharmacology ; Pediatrics ; Pharmacokinetics ; Pharmacology & Pharmacy ; Polymer blends ; Polymer films ; Polymers ; Polyvinyl alcohol ; Potassium ; Propanolol hydrochloride ; Propranolol ; Propranolol - administration & dosage ; Propranolol - pharmacokinetics ; Propranolol - pharmacology ; Rabbits ; Science & Technology ; Spectrum analysis ; Tablets</subject><ispartof>Drug design, development and therapy, 2020-01, Vol.14, p.4277-4289</ispartof><rights>2020 Mohamad et al.</rights><rights>COPYRIGHT 2020 Dove Medical Press Limited</rights><rights>2020. This work is licensed under https://creativecommons.org/licenses/by-nc/3.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2020 Mohamad et al. 2020 Mohamad et al.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>true</woscitedreferencessubscribed><woscitedreferencescount>14</woscitedreferencescount><woscitedreferencesoriginalsourcerecordid>wos000577502900001</woscitedreferencesoriginalsourcerecordid><citedby>FETCH-LOGICAL-c576t-dcc2b9531bad5c0bd62fe9d02f8dcff1b14be462d30ad9d8309e2e46fe3557803</citedby><cites>FETCH-LOGICAL-c576t-dcc2b9531bad5c0bd62fe9d02f8dcff1b14be462d30ad9d8309e2e46fe3557803</cites><orcidid>0000-0002-6467-849X ; 0000-0002-2948-1691</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7573323/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7573323/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,315,728,781,785,865,886,2103,2115,3863,27929,27930,28253,53796,53798</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33116415$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Mohamad, Soad A.</creatorcontrib><creatorcontrib>Salem, Hesham</creatorcontrib><creatorcontrib>Yassin, Heba A.</creatorcontrib><creatorcontrib>Mansour, Heba F.</creatorcontrib><title>Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation</title><title>Drug design, development and therapy</title><addtitle>DRUG DES DEV THER</addtitle><addtitle>Drug Des Devel Ther</addtitle><description>Objective: To formulate and assess bucco-adhesive films of propranolol hydrochloride for pediatric use.
Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared films were physically investigated for variation of weight, propranolol content, thickness, surface pH, proportion of moisture, folding endurance and mucoadhesion. In vitro drug release study and kinetic analysis of the corresponding data have been conducted. The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method. The pharmacokinetic parameters of the drug were calculated following administration of the optimized film and the corresponding marketed oral tablets to albino rabbits.
Key Finding: The compatibility study revealed the absence of drug/polymer interaction. The film formulations had suitable mucoadhesive and mechanical properties. The optimized formulation exhibited reasonable drug release that followed Higuchi diffusion pattern. The calculated AUC0-8h presented an enhancement in the bioavailability of propranolol hydrochloride from the selected film formulation by 1.9 times relative to the marketed propranolol oral tablets.
Conclusion: These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery.</description><subject>Adhesion tests</subject><subject>Adhesiveness</subject><subject>Adhesives</subject><subject>Administration, Buccal</subject><subject>Adrenergic beta-Antagonists - administration & dosage</subject><subject>Adrenergic beta-Antagonists - chemistry</subject><subject>Adrenergic beta-Antagonists - pharmacology</subject><subject>Animals</subject><subject>Area Under Curve</subject><subject>Bioavailability</subject><subject>Biocompatibility</subject><subject>Biological Availability</subject><subject>buccoadhesive</subject><subject>Calorimetry</subject><subject>Cheek</subject><subject>Chemistry, Medicinal</subject><subject>Child</subject><subject>Chitosan</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Differential scanning calorimetry</subject><subject>Dosage</subject><subject>Dosage Forms</subject><subject>Drug Compounding</subject><subject>Drug delivery systems</subject><subject>Drug dosages</subject><subject>Excipients</subject><subject>Fourier analysis</subject><subject>Fourier transforms</subject><subject>High-performance liquid chromatography</subject><subject>hplc</subject><subject>Humans</subject><subject>Hydrogen-Ion Concentration</subject><subject>Infant</subject><subject>Infrared spectroscopy</subject><subject>Investigations</subject><subject>Life Sciences & Biomedicine</subject><subject>Liquid chromatography</subject><subject>Mathematical analysis</subject><subject>Mechanical properties</subject><subject>Moisture content</subject><subject>Mucin</subject><subject>Oral administration</subject><subject>Original Research</subject><subject>paediatric</subject><subject>Patient compliance</subject><subject>Pediatric pharmacology</subject><subject>Pediatrics</subject><subject>Pharmacokinetics</subject><subject>Pharmacology & Pharmacy</subject><subject>Polymer blends</subject><subject>Polymer films</subject><subject>Polymers</subject><subject>Polyvinyl alcohol</subject><subject>Potassium</subject><subject>Propanolol hydrochloride</subject><subject>Propranolol</subject><subject>Propranolol - administration & dosage</subject><subject>Propranolol - pharmacokinetics</subject><subject>Propranolol - pharmacology</subject><subject>Rabbits</subject><subject>Science & Technology</subject><subject>Spectrum analysis</subject><subject>Tablets</subject><issn>1177-8881</issn><issn>1177-8881</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2020</creationdate><recordtype>article</recordtype><sourceid>AOWDO</sourceid><sourceid>EIF</sourceid><sourceid>8G5</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><sourceid>GUQSH</sourceid><sourceid>M2O</sourceid><sourceid>DOA</sourceid><recordid>eNqNkl1rFDEUhgdRbK3eeS0BQQTdNZ-TGS-EutvaQsFC63XIJJndlOycmsys7E_wX5vp1rorXkgukpzznDfknLcoXhI8pYTLD_P5_Hp6RUvJiHxUHBIi5aSqKvJ453xQPEvpBuOSlRQ_LQ4YI6TkRBwWPz8PxsDk2C5d8muHTn1YIZ2QRpfOet1Hb9BlhFsX0RySXmQC4gq1ENHVJvVulfNzF3Jp3CBo79ioOwgQ0NnGRjDLANFb9xGdd5O17yMg3Vnkx8sa0Mlah0H3HrrnxZNWh-Re3O9HxbfTk-vZ2eTi65fz2fHFxAhZ9hNrDG1qwUijrTC4sSVtXW0xbStr2pY0hDeOl9QyrG1tK4ZrR3OgdUwIWWF2VJxvdS3oG3Ub_UrHjQLt1V0A4kLp2HsTnKqdsWWpOaOSc211YxhvG8ow53UjKp21Pm21bodm5axxXR912BPdz3R-qRawVlJIxijLAm_vBSJ8H1zq1con40LQnYMhKcqFqBivmMjo67_QGxhil1s1UkSUUlbVH2qh8wd810J-14yi6rjklPG6pCM1_QeVlx0HCp1rfY7vFbzZKVg6HfplgjCMg0v74PstaCKkFF370AyC1ehXNfpV3fs14692G_gA_zZoBt5tgR-ugTYZ7zrjHjCMsZBSYFrnEyaZrv6fnvn-zngzGLqe_QL33AZK</recordid><startdate>20200101</startdate><enddate>20200101</enddate><creator>Mohamad, Soad A.</creator><creator>Salem, Hesham</creator><creator>Yassin, Heba A.</creator><creator>Mansour, Heba F.</creator><general>Dove Medical Press Ltd</general><general>Dove Medical Press Limited</general><general>Taylor & Francis Ltd</general><general>Dove</general><general>Dove Medical Press</general><scope>AOWDO</scope><scope>BLEPL</scope><scope>DTL</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>7QO</scope><scope>7RV</scope><scope>7XB</scope><scope>8FD</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>8G5</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BENPR</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>GUQSH</scope><scope>KB0</scope><scope>M2O</scope><scope>MBDVC</scope><scope>NAPCQ</scope><scope>P64</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>Q9U</scope><scope>7X8</scope><scope>5PM</scope><scope>DOA</scope><orcidid>https://orcid.org/0000-0002-6467-849X</orcidid><orcidid>https://orcid.org/0000-0002-2948-1691</orcidid></search><sort><creationdate>20200101</creationdate><title>Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation</title><author>Mohamad, Soad A. ; Salem, Hesham ; Yassin, Heba A. ; Mansour, Heba F.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c576t-dcc2b9531bad5c0bd62fe9d02f8dcff1b14be462d30ad9d8309e2e46fe3557803</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2020</creationdate><topic>Adhesion tests</topic><topic>Adhesiveness</topic><topic>Adhesives</topic><topic>Administration, Buccal</topic><topic>Adrenergic beta-Antagonists - administration & dosage</topic><topic>Adrenergic beta-Antagonists - chemistry</topic><topic>Adrenergic beta-Antagonists - pharmacology</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Bioavailability</topic><topic>Biocompatibility</topic><topic>Biological Availability</topic><topic>buccoadhesive</topic><topic>Calorimetry</topic><topic>Cheek</topic><topic>Chemistry, Medicinal</topic><topic>Child</topic><topic>Chitosan</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Differential scanning calorimetry</topic><topic>Dosage</topic><topic>Dosage Forms</topic><topic>Drug Compounding</topic><topic>Drug delivery systems</topic><topic>Drug dosages</topic><topic>Excipients</topic><topic>Fourier analysis</topic><topic>Fourier transforms</topic><topic>High-performance liquid chromatography</topic><topic>hplc</topic><topic>Humans</topic><topic>Hydrogen-Ion Concentration</topic><topic>Infant</topic><topic>Infrared spectroscopy</topic><topic>Investigations</topic><topic>Life Sciences & Biomedicine</topic><topic>Liquid chromatography</topic><topic>Mathematical analysis</topic><topic>Mechanical properties</topic><topic>Moisture content</topic><topic>Mucin</topic><topic>Oral administration</topic><topic>Original Research</topic><topic>paediatric</topic><topic>Patient compliance</topic><topic>Pediatric pharmacology</topic><topic>Pediatrics</topic><topic>Pharmacokinetics</topic><topic>Pharmacology & Pharmacy</topic><topic>Polymer blends</topic><topic>Polymer films</topic><topic>Polymers</topic><topic>Polyvinyl alcohol</topic><topic>Potassium</topic><topic>Propanolol hydrochloride</topic><topic>Propranolol</topic><topic>Propranolol - administration & dosage</topic><topic>Propranolol - pharmacokinetics</topic><topic>Propranolol - pharmacology</topic><topic>Rabbits</topic><topic>Science & Technology</topic><topic>Spectrum analysis</topic><topic>Tablets</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Mohamad, Soad A.</creatorcontrib><creatorcontrib>Salem, Hesham</creatorcontrib><creatorcontrib>Yassin, Heba A.</creatorcontrib><creatorcontrib>Mansour, Heba F.</creatorcontrib><collection>Web of Science - Science Citation Index Expanded - 2020</collection><collection>Web of Science Core Collection</collection><collection>Science Citation Index Expanded</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>Biotechnology Research Abstracts</collection><collection>Nursing & Allied Health Database</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Technology Research Database</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Research Library (Alumni Edition)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>ProQuest Central</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Engineering Research Database</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>Research Library Prep</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Research Library</collection><collection>Research Library (Corporate)</collection><collection>Nursing & Allied Health Premium</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Access via ProQuest (Open Access)</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>ProQuest Central Basic</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><collection>DOAJ Directory of Open Access Journals</collection><jtitle>Drug design, development and therapy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Mohamad, Soad A.</au><au>Salem, Hesham</au><au>Yassin, Heba A.</au><au>Mansour, Heba F.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation</atitle><jtitle>Drug design, development and therapy</jtitle><stitle>DRUG DES DEV THER</stitle><addtitle>Drug Des Devel Ther</addtitle><date>2020-01-01</date><risdate>2020</risdate><volume>14</volume><spage>4277</spage><epage>4289</epage><pages>4277-4289</pages><issn>1177-8881</issn><eissn>1177-8881</eissn><abstract>Objective: To formulate and assess bucco-adhesive films of propranolol hydrochloride for pediatric use.
Methods: Different films were formulated adopting mucin, polyvinyl alcohol, chitosan and carbopol. A drug/polymer compatibility study was conducted adopting differential scanning calorimetry and Fourier transform infrared spectroscopy. The prepared films were physically investigated for variation of weight, propranolol content, thickness, surface pH, proportion of moisture, folding endurance and mucoadhesion. In vitro drug release study and kinetic analysis of the corresponding data have been conducted. The optimized formulation was selected for a bioavailability study using albino rabbits and adopting a developed HPLC method. The pharmacokinetic parameters of the drug were calculated following administration of the optimized film and the corresponding marketed oral tablets to albino rabbits.
Key Finding: The compatibility study revealed the absence of drug/polymer interaction. The film formulations had suitable mucoadhesive and mechanical properties. The optimized formulation exhibited reasonable drug release that followed Higuchi diffusion pattern. The calculated AUC0-8h presented an enhancement in the bioavailability of propranolol hydrochloride from the selected film formulation by 1.9 times relative to the marketed propranolol oral tablets.
Conclusion: These findings support that propranolol hydrochloride bucco-adhesive film can be considered as a proper effective dosage form for pediatric delivery.</abstract><cop>ALBANY</cop><pub>Dove Medical Press Ltd</pub><pmid>33116415</pmid><doi>10.2147/DDDT.S267317</doi><tpages>13</tpages><orcidid>https://orcid.org/0000-0002-6467-849X</orcidid><orcidid>https://orcid.org/0000-0002-2948-1691</orcidid><oa>free_for_read</oa></addata></record> |
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subjects | Adhesion tests Adhesiveness Adhesives Administration, Buccal Adrenergic beta-Antagonists - administration & dosage Adrenergic beta-Antagonists - chemistry Adrenergic beta-Antagonists - pharmacology Animals Area Under Curve Bioavailability Biocompatibility Biological Availability buccoadhesive Calorimetry Cheek Chemistry, Medicinal Child Chitosan Chromatography, High Pressure Liquid Differential scanning calorimetry Dosage Dosage Forms Drug Compounding Drug delivery systems Drug dosages Excipients Fourier analysis Fourier transforms High-performance liquid chromatography hplc Humans Hydrogen-Ion Concentration Infant Infrared spectroscopy Investigations Life Sciences & Biomedicine Liquid chromatography Mathematical analysis Mechanical properties Moisture content Mucin Oral administration Original Research paediatric Patient compliance Pediatric pharmacology Pediatrics Pharmacokinetics Pharmacology & Pharmacy Polymer blends Polymer films Polymers Polyvinyl alcohol Potassium Propanolol hydrochloride Propranolol Propranolol - administration & dosage Propranolol - pharmacokinetics Propranolol - pharmacology Rabbits Science & Technology Spectrum analysis Tablets |
title | Bucco-Adhesive Film as a Pediatric Proper Dosage Form for Systemic Delivery of Propranolol Hydrochloride: In-vitro and in-vivo Evaluation |
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