Development and optimization of ganciclovir-loaded carbopol topical gel by response surface methodology for enhanced skin permeation
Low permeability is one of the barriers to the bioavailability of drugs through the oral route. The purpose of the present study was to design and optimize a sustained release and highly permeable hydrogel formulation of ganciclovir (GCV) by using response surface methodology (RSM). Carbopol 934P wa...
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| Veröffentlicht in: | Polymer bulletin (Berlin, Germany) Germany), 2023-11, Vol.80 (11), p.11817-11844 |
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| creator | Siddique, Waqar Zaman, Muhammad Waheed, Sadaf Sarfraz, Rai Muhammad Bashir, Sajid Minhas, Muhammad Usman Farooq, Umar Saeed, Asad |
| description | Low permeability is one of the barriers to the bioavailability of drugs through the oral route. The purpose of the present study was to design and optimize a sustained release and highly permeable hydrogel formulation of ganciclovir (GCV) by using response surface methodology (RSM). Carbopol 934P was used as a gelling agent, with two permeation enhancers, i.e., propylene glycol (PG) and oleic acid (OA), which were selected as variables
X
1
and
X
2
, respectively. A total number of 13 runs prepared by using a central composite rotatable design (CCRD), followed by the preparation and evaluation of various parameters, including flux, lag time,
K
p
,
and the rheological studies were evaluated. FTIR analysis showed that there was no interaction between the drug, polymer, and other excipients. The outcomes of
ex vivo
permeation studies have reviled that the values of flux, lag time, and
k
p
were found to be 2.08800 ± 0.008, −6.982638 ± 0.01, −2.6917 ± 1.21, −29.7116 ± 0.68, and 0.00020, −0.00069, respectively. The spreadability index and the viscosity of the gel formulations were between the range of 2.63 ± 0.12–3.50 ± 0.08 and 5013.66 ± 1.69–5077.66 ± 2.05, respectively. On the other hand, the pH of all preparations was maintained at 7.02–7.13 pH to avoid skin irritation. After evaluating the said parameters, the composition for the optimized formulation is PG 5gm, OA 0.4gm, and carbopol 0.5gm. Furthermore, the findings have advocated that the hydrogels could be used, not only to deliver the drug in a sustained manner but also to improve the permeation of the drug and hence its bioavailability. |
| doi_str_mv | 10.1007/s00289-022-04612-5 |
| format | Article |
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X
1
and
X
2
, respectively. A total number of 13 runs prepared by using a central composite rotatable design (CCRD), followed by the preparation and evaluation of various parameters, including flux, lag time,
K
p
,
and the rheological studies were evaluated. FTIR analysis showed that there was no interaction between the drug, polymer, and other excipients. The outcomes of
ex vivo
permeation studies have reviled that the values of flux, lag time, and
k
p
were found to be 2.08800 ± 0.008, −6.982638 ± 0.01, −2.6917 ± 1.21, −29.7116 ± 0.68, and 0.00020, −0.00069, respectively. The spreadability index and the viscosity of the gel formulations were between the range of 2.63 ± 0.12–3.50 ± 0.08 and 5013.66 ± 1.69–5077.66 ± 2.05, respectively. On the other hand, the pH of all preparations was maintained at 7.02–7.13 pH to avoid skin irritation. After evaluating the said parameters, the composition for the optimized formulation is PG 5gm, OA 0.4gm, and carbopol 0.5gm. Furthermore, the findings have advocated that the hydrogels could be used, not only to deliver the drug in a sustained manner but also to improve the permeation of the drug and hence its bioavailability.</description><identifier>ISSN: 0170-0839</identifier><identifier>EISSN: 1436-2449</identifier><identifier>DOI: 10.1007/s00289-022-04612-5</identifier><language>eng</language><publisher>Berlin/Heidelberg: Springer Berlin Heidelberg</publisher><subject>Bioavailability ; Characterization and Evaluation of Materials ; Chemicals ; Chemistry ; Chemistry and Materials Science ; Complex Fluids and Microfluidics ; Design ; Design optimization ; Drug delivery systems ; Fourier transforms ; Hydrogels ; Irritation ; Laboratories ; Lag time ; Lipids ; Oleic acid ; Optimization ; Organic Chemistry ; Original Paper ; Parameters ; Permeation ; Physical Chemistry ; Polymer Sciences ; Propylene ; Response surface methodology ; Rheological properties ; Skin ; Soft and Granular Matter ; Solvents ; Sustained release ; Transdermal medication ; Viscosity</subject><ispartof>Polymer bulletin (Berlin, Germany), 2023-11, Vol.80 (11), p.11817-11844</ispartof><rights>The Author(s), under exclusive licence to Springer-Verlag GmbH Germany, part of Springer Nature 2022. Springer Nature or its licensor (e.g. a society or other partner) holds exclusive rights to this article under a publishing agreement with the author(s) or other rightsholder(s); author self-archiving of the accepted manuscript version of this article is solely governed by the terms of such publishing agreement and applicable law.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c319t-326c1739000bb79d7105fdbb207e9d1fdedf1776654124d879c8c088ef6c3373</citedby><cites>FETCH-LOGICAL-c319t-326c1739000bb79d7105fdbb207e9d1fdedf1776654124d879c8c088ef6c3373</cites><orcidid>0000-0001-7302-4175</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://link.springer.com/content/pdf/10.1007/s00289-022-04612-5$$EPDF$$P50$$Gspringer$$H</linktopdf><linktohtml>$$Uhttps://www.proquest.com/docview/2917934570?pq-origsite=primo$$EHTML$$P50$$Gproquest$$H</linktohtml><link.rule.ids>315,782,786,21397,27933,27934,33753,41497,42566,43814,51328,64394,64398,72478</link.rule.ids></links><search><creatorcontrib>Siddique, Waqar</creatorcontrib><creatorcontrib>Zaman, Muhammad</creatorcontrib><creatorcontrib>Waheed, Sadaf</creatorcontrib><creatorcontrib>Sarfraz, Rai Muhammad</creatorcontrib><creatorcontrib>Bashir, Sajid</creatorcontrib><creatorcontrib>Minhas, Muhammad Usman</creatorcontrib><creatorcontrib>Farooq, Umar</creatorcontrib><creatorcontrib>Saeed, Asad</creatorcontrib><title>Development and optimization of ganciclovir-loaded carbopol topical gel by response surface methodology for enhanced skin permeation</title><title>Polymer bulletin (Berlin, Germany)</title><addtitle>Polym. Bull</addtitle><description>Low permeability is one of the barriers to the bioavailability of drugs through the oral route. The purpose of the present study was to design and optimize a sustained release and highly permeable hydrogel formulation of ganciclovir (GCV) by using response surface methodology (RSM). Carbopol 934P was used as a gelling agent, with two permeation enhancers, i.e., propylene glycol (PG) and oleic acid (OA), which were selected as variables
X
1
and
X
2
, respectively. A total number of 13 runs prepared by using a central composite rotatable design (CCRD), followed by the preparation and evaluation of various parameters, including flux, lag time,
K
p
,
and the rheological studies were evaluated. FTIR analysis showed that there was no interaction between the drug, polymer, and other excipients. The outcomes of
ex vivo
permeation studies have reviled that the values of flux, lag time, and
k
p
were found to be 2.08800 ± 0.008, −6.982638 ± 0.01, −2.6917 ± 1.21, −29.7116 ± 0.68, and 0.00020, −0.00069, respectively. The spreadability index and the viscosity of the gel formulations were between the range of 2.63 ± 0.12–3.50 ± 0.08 and 5013.66 ± 1.69–5077.66 ± 2.05, respectively. On the other hand, the pH of all preparations was maintained at 7.02–7.13 pH to avoid skin irritation. After evaluating the said parameters, the composition for the optimized formulation is PG 5gm, OA 0.4gm, and carbopol 0.5gm. Furthermore, the findings have advocated that the hydrogels could be used, not only to deliver the drug in a sustained manner but also to improve the permeation of the drug and hence its bioavailability.</description><subject>Bioavailability</subject><subject>Characterization and Evaluation of Materials</subject><subject>Chemicals</subject><subject>Chemistry</subject><subject>Chemistry and Materials Science</subject><subject>Complex Fluids and Microfluidics</subject><subject>Design</subject><subject>Design optimization</subject><subject>Drug delivery systems</subject><subject>Fourier transforms</subject><subject>Hydrogels</subject><subject>Irritation</subject><subject>Laboratories</subject><subject>Lag time</subject><subject>Lipids</subject><subject>Oleic acid</subject><subject>Optimization</subject><subject>Organic Chemistry</subject><subject>Original Paper</subject><subject>Parameters</subject><subject>Permeation</subject><subject>Physical Chemistry</subject><subject>Polymer Sciences</subject><subject>Propylene</subject><subject>Response surface methodology</subject><subject>Rheological properties</subject><subject>Skin</subject><subject>Soft and Granular Matter</subject><subject>Solvents</subject><subject>Sustained release</subject><subject>Transdermal medication</subject><subject>Viscosity</subject><issn>0170-0839</issn><issn>1436-2449</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><recordid>eNp9kEFv1DAQhS0EEkvhD3Cy1LNhbCdxfEQttEiVuPRuOc54mzbxpHa20nLuD8d0K3HjNBrpve_NPMY-S_giAczXAqB6K0ApAU0nlWjfsJ1sdCdU09i3bAfSgIBe2_fsQyn3UPeukzv2fIlPONO6YNq4TyOndZuW6bffJkqcIt_7FKYw09OUxUx-xJEHnwdaaeYbrVPwM9_jzIcjz1hWSgV5OeToA_IFtzsaaab9kUfKHNNdpVVCeZgSXzEv-JLzkb2Lfi746XWesdsf328vrsXNr6ufF99uRNDSbkKrLkijLQAMg7GjkdDGcRgUGLSjjPW2KE39q22kasbe2NAH6HuMXdDa6DN2fsKumR4PWDZ3T4ecaqJTVhqrm9ZAVamTKmQqJWN0a54Wn49OgvtbtjuV7WrZ7qVs11aTPplKFac95n_o_7j-AEPDhNk</recordid><startdate>20231101</startdate><enddate>20231101</enddate><creator>Siddique, Waqar</creator><creator>Zaman, Muhammad</creator><creator>Waheed, Sadaf</creator><creator>Sarfraz, Rai Muhammad</creator><creator>Bashir, Sajid</creator><creator>Minhas, Muhammad Usman</creator><creator>Farooq, Umar</creator><creator>Saeed, Asad</creator><general>Springer Berlin Heidelberg</general><general>Springer Nature B.V</general><scope>AAYXX</scope><scope>CITATION</scope><scope>8FE</scope><scope>8FG</scope><scope>ABJCF</scope><scope>AFKRA</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>HCIFZ</scope><scope>KB.</scope><scope>PDBOC</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><orcidid>https://orcid.org/0000-0001-7302-4175</orcidid></search><sort><creationdate>20231101</creationdate><title>Development and optimization of ganciclovir-loaded carbopol topical gel by response surface methodology for enhanced skin permeation</title><author>Siddique, Waqar ; Zaman, Muhammad ; Waheed, Sadaf ; Sarfraz, Rai Muhammad ; Bashir, Sajid ; Minhas, Muhammad Usman ; Farooq, Umar ; Saeed, Asad</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c319t-326c1739000bb79d7105fdbb207e9d1fdedf1776654124d879c8c088ef6c3373</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><topic>Bioavailability</topic><topic>Characterization and Evaluation of Materials</topic><topic>Chemicals</topic><topic>Chemistry</topic><topic>Chemistry and Materials Science</topic><topic>Complex Fluids and Microfluidics</topic><topic>Design</topic><topic>Design optimization</topic><topic>Drug delivery systems</topic><topic>Fourier transforms</topic><topic>Hydrogels</topic><topic>Irritation</topic><topic>Laboratories</topic><topic>Lag time</topic><topic>Lipids</topic><topic>Oleic acid</topic><topic>Optimization</topic><topic>Organic Chemistry</topic><topic>Original Paper</topic><topic>Parameters</topic><topic>Permeation</topic><topic>Physical Chemistry</topic><topic>Polymer Sciences</topic><topic>Propylene</topic><topic>Response surface methodology</topic><topic>Rheological properties</topic><topic>Skin</topic><topic>Soft and Granular Matter</topic><topic>Solvents</topic><topic>Sustained release</topic><topic>Transdermal medication</topic><topic>Viscosity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Siddique, Waqar</creatorcontrib><creatorcontrib>Zaman, Muhammad</creatorcontrib><creatorcontrib>Waheed, Sadaf</creatorcontrib><creatorcontrib>Sarfraz, Rai Muhammad</creatorcontrib><creatorcontrib>Bashir, Sajid</creatorcontrib><creatorcontrib>Minhas, Muhammad Usman</creatorcontrib><creatorcontrib>Farooq, Umar</creatorcontrib><creatorcontrib>Saeed, Asad</creatorcontrib><collection>CrossRef</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Technology Collection</collection><collection>Materials Science & Engineering Collection</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central</collection><collection>Technology Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Materials Science Collection</collection><collection>ProQuest Central Korea</collection><collection>SciTech Premium Collection</collection><collection>Materials Science Database</collection><collection>Materials Science Collection</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><jtitle>Polymer bulletin (Berlin, Germany)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Siddique, Waqar</au><au>Zaman, Muhammad</au><au>Waheed, Sadaf</au><au>Sarfraz, Rai Muhammad</au><au>Bashir, Sajid</au><au>Minhas, Muhammad Usman</au><au>Farooq, Umar</au><au>Saeed, Asad</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development and optimization of ganciclovir-loaded carbopol topical gel by response surface methodology for enhanced skin permeation</atitle><jtitle>Polymer bulletin (Berlin, Germany)</jtitle><stitle>Polym. Bull</stitle><date>2023-11-01</date><risdate>2023</risdate><volume>80</volume><issue>11</issue><spage>11817</spage><epage>11844</epage><pages>11817-11844</pages><issn>0170-0839</issn><eissn>1436-2449</eissn><abstract>Low permeability is one of the barriers to the bioavailability of drugs through the oral route. The purpose of the present study was to design and optimize a sustained release and highly permeable hydrogel formulation of ganciclovir (GCV) by using response surface methodology (RSM). Carbopol 934P was used as a gelling agent, with two permeation enhancers, i.e., propylene glycol (PG) and oleic acid (OA), which were selected as variables
X
1
and
X
2
, respectively. A total number of 13 runs prepared by using a central composite rotatable design (CCRD), followed by the preparation and evaluation of various parameters, including flux, lag time,
K
p
,
and the rheological studies were evaluated. FTIR analysis showed that there was no interaction between the drug, polymer, and other excipients. The outcomes of
ex vivo
permeation studies have reviled that the values of flux, lag time, and
k
p
were found to be 2.08800 ± 0.008, −6.982638 ± 0.01, −2.6917 ± 1.21, −29.7116 ± 0.68, and 0.00020, −0.00069, respectively. The spreadability index and the viscosity of the gel formulations were between the range of 2.63 ± 0.12–3.50 ± 0.08 and 5013.66 ± 1.69–5077.66 ± 2.05, respectively. On the other hand, the pH of all preparations was maintained at 7.02–7.13 pH to avoid skin irritation. After evaluating the said parameters, the composition for the optimized formulation is PG 5gm, OA 0.4gm, and carbopol 0.5gm. Furthermore, the findings have advocated that the hydrogels could be used, not only to deliver the drug in a sustained manner but also to improve the permeation of the drug and hence its bioavailability.</abstract><cop>Berlin/Heidelberg</cop><pub>Springer Berlin Heidelberg</pub><doi>10.1007/s00289-022-04612-5</doi><tpages>28</tpages><orcidid>https://orcid.org/0000-0001-7302-4175</orcidid></addata></record> |
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| subjects | Bioavailability Characterization and Evaluation of Materials Chemicals Chemistry Chemistry and Materials Science Complex Fluids and Microfluidics Design Design optimization Drug delivery systems Fourier transforms Hydrogels Irritation Laboratories Lag time Lipids Oleic acid Optimization Organic Chemistry Original Paper Parameters Permeation Physical Chemistry Polymer Sciences Propylene Response surface methodology Rheological properties Skin Soft and Granular Matter Solvents Sustained release Transdermal medication Viscosity |
| title | Development and optimization of ganciclovir-loaded carbopol topical gel by response surface methodology for enhanced skin permeation |
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