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Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability
Utilization of lipid-based drug delivery systems has recently gained focus for drugs characterized by poor aqueous solubility. The improved aqueous solubility overcomes one of the main barriers that limit their bioavailability. The objective of this work was to improve the solubility and oral bioava...
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| Published in: | AAPS PharmSciTech 2015-02, Vol.16 (1), p.53-58 |
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| creator | Fahmy, Usama A. Ahmed, Osama A. A. Hosny, Khaled M. |
| description | Utilization of lipid-based drug delivery systems has recently gained focus for drugs characterized by poor aqueous solubility. The improved aqueous solubility overcomes one of the main barriers that limit their bioavailability. The objective of this work was to improve the solubility and oral bioavailability of Avanafil (AVA), a recently approved second generation type 5 phospodiesterase inhibitor used for erectile dysfunction.AVA was formulated as self-nanoemulsifying drug delivery system (SNEDDS) utilizing various oils, surfactants, and cosurfactants. The solubility of AVA in various oils, surfactants, and cosurfactants was determined. Ternary phase diagram was constructed to identify stable nanoemulsion region. The prepared AVA loaded SNEDDS were assessed for optical clarity, droplet size, conductivity, and stability studies.
In vitro
drug release and
in vivo
pharmacokinetic parameters using animal model were also investigated. Results revealed that stable AVA (SNEDDS) were successfully developed with a droplet size range of 65 to 190 nm. SNEDDS composed of 25% dill oil, 55% Tween 80, and 20% propylene glycol successfully improved solubilization of AVA (over 80% within 30 min) vis-a-vis the powder AVA (35% within 30 min).
In vivo
pharmacokinetic showed a significant (
P
|
| doi_str_mv | 10.1208/s12249-014-0199-3 |
| format | article |
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In vitro
drug release and
in vivo
pharmacokinetic parameters using animal model were also investigated. Results revealed that stable AVA (SNEDDS) were successfully developed with a droplet size range of 65 to 190 nm. SNEDDS composed of 25% dill oil, 55% Tween 80, and 20% propylene glycol successfully improved solubilization of AVA (over 80% within 30 min) vis-a-vis the powder AVA (35% within 30 min).
In vivo
pharmacokinetic showed a significant (
P
< 0.05) increase in C
max
, reduction in T
max
, and SNEDDS enhanced the bioavailability in the rats by 1.4-fold when compared with pure drug.</description><identifier>ISSN: 1530-9932</identifier><identifier>EISSN: 1530-9932</identifier><identifier>DOI: 10.1208/s12249-014-0199-3</identifier><identifier>PMID: 25168449</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Administration, Oral ; Animals ; Biochemistry ; Biological Availability ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; Diffusion ; Drug Compounding - methods ; Drug Stability ; Emulsifying Agents - chemistry ; Emulsions ; Male ; Metabolic Clearance Rate ; Nanocapsules - administration & dosage ; Nanocapsules - chemistry ; Nanocapsules - ultrastructure ; Particle Size ; Pharmacology/Toxicology ; Pharmacy ; Phase Transition ; Pyrimidines - administration & dosage ; Pyrimidines - blood ; Pyrimidines - chemistry ; Pyrimidines - pharmacokinetics ; Rats ; Rats, Wistar ; Research Article</subject><ispartof>AAPS PharmSciTech, 2015-02, Vol.16 (1), p.53-58</ispartof><rights>American Association of Pharmaceutical Scientists 2014</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c545t-13e33213a7ae38ce508c4198a1515fc44a536944afed243dc837809034a5d77d3</citedby><cites>FETCH-LOGICAL-c545t-13e33213a7ae38ce508c4198a1515fc44a536944afed243dc837809034a5d77d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4309810/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4309810/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/25168449$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Fahmy, Usama A.</creatorcontrib><creatorcontrib>Ahmed, Osama A. A.</creatorcontrib><creatorcontrib>Hosny, Khaled M.</creatorcontrib><title>Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>Utilization of lipid-based drug delivery systems has recently gained focus for drugs characterized by poor aqueous solubility. The improved aqueous solubility overcomes one of the main barriers that limit their bioavailability. The objective of this work was to improve the solubility and oral bioavailability of Avanafil (AVA), a recently approved second generation type 5 phospodiesterase inhibitor used for erectile dysfunction.AVA was formulated as self-nanoemulsifying drug delivery system (SNEDDS) utilizing various oils, surfactants, and cosurfactants. The solubility of AVA in various oils, surfactants, and cosurfactants was determined. Ternary phase diagram was constructed to identify stable nanoemulsion region. The prepared AVA loaded SNEDDS were assessed for optical clarity, droplet size, conductivity, and stability studies.
In vitro
drug release and
in vivo
pharmacokinetic parameters using animal model were also investigated. Results revealed that stable AVA (SNEDDS) were successfully developed with a droplet size range of 65 to 190 nm. SNEDDS composed of 25% dill oil, 55% Tween 80, and 20% propylene glycol successfully improved solubilization of AVA (over 80% within 30 min) vis-a-vis the powder AVA (35% within 30 min).
In vivo
pharmacokinetic showed a significant (
P
< 0.05) increase in C
max
, reduction in T
max
, and SNEDDS enhanced the bioavailability in the rats by 1.4-fold when compared with pure drug.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Biochemistry</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Diffusion</subject><subject>Drug Compounding - methods</subject><subject>Drug Stability</subject><subject>Emulsifying Agents - chemistry</subject><subject>Emulsions</subject><subject>Male</subject><subject>Metabolic Clearance Rate</subject><subject>Nanocapsules - administration & dosage</subject><subject>Nanocapsules - chemistry</subject><subject>Nanocapsules - ultrastructure</subject><subject>Particle Size</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Phase Transition</subject><subject>Pyrimidines - administration & dosage</subject><subject>Pyrimidines - blood</subject><subject>Pyrimidines - chemistry</subject><subject>Pyrimidines - pharmacokinetics</subject><subject>Rats</subject><subject>Rats, Wistar</subject><subject>Research Article</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><recordid>eNp9kctu1DAUhi0Eohd4ADbISzYpvmUm3iCVXgCpUqW2rK1T52TGlWMPdhKUN-Cx65kpVdmwsI-l_z_fsf0T8oGzEy5Y8zlzIZSuGFdlaV3JV-SQ15JVWkvx-sX5gBzl_MCYkFzLt-RA1HzRKKUPyZ9znNDHTY9hoBBaejGBH2FwMdDY0dMJAnTO01v0XRUgROxHn103u7Ci52ksG3o3YZrp7ZwH7OlvN6zpDWxcS69DxmGHsTvgjh_WECy29KuLMIHzcO-8G-Z35E0HPuP7p3pMfl5e3J19r66uv_04O72qbK3qoeISpRRcwhJQNhZr1ljFdQO85nVnlYJaLnQpHbZCydY2ctkwzWQR2uWylcfky567Ge97bG15dwJvNsn1kGYTwZl_leDWZhUnoyTTDWcF8OkJkOKvEfNgepcteg8B45gNXyyYYkJLWax8b7Up5pywex7DmdkmaPYJmpKg2SZotj0fX97vueNvZMUg9oZcpLDCZB7imEL5s_9QHwHGAqkq</recordid><startdate>20150201</startdate><enddate>20150201</enddate><creator>Fahmy, Usama A.</creator><creator>Ahmed, Osama A. A.</creator><creator>Hosny, Khaled M.</creator><general>Springer US</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>5PM</scope></search><sort><creationdate>20150201</creationdate><title>Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability</title><author>Fahmy, Usama A. ; Ahmed, Osama A. A. ; Hosny, Khaled M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c545t-13e33213a7ae38ce508c4198a1515fc44a536944afed243dc837809034a5d77d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Biochemistry</topic><topic>Biological Availability</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Diffusion</topic><topic>Drug Compounding - methods</topic><topic>Drug Stability</topic><topic>Emulsifying Agents - chemistry</topic><topic>Emulsions</topic><topic>Male</topic><topic>Metabolic Clearance Rate</topic><topic>Nanocapsules - administration & dosage</topic><topic>Nanocapsules - chemistry</topic><topic>Nanocapsules - ultrastructure</topic><topic>Particle Size</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Phase Transition</topic><topic>Pyrimidines - administration & dosage</topic><topic>Pyrimidines - blood</topic><topic>Pyrimidines - chemistry</topic><topic>Pyrimidines - pharmacokinetics</topic><topic>Rats</topic><topic>Rats, Wistar</topic><topic>Research Article</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Fahmy, Usama A.</creatorcontrib><creatorcontrib>Ahmed, Osama A. A.</creatorcontrib><creatorcontrib>Hosny, Khaled M.</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Fahmy, Usama A.</au><au>Ahmed, Osama A. A.</au><au>Hosny, Khaled M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2015-02-01</date><risdate>2015</risdate><volume>16</volume><issue>1</issue><spage>53</spage><epage>58</epage><pages>53-58</pages><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>Utilization of lipid-based drug delivery systems has recently gained focus for drugs characterized by poor aqueous solubility. The improved aqueous solubility overcomes one of the main barriers that limit their bioavailability. The objective of this work was to improve the solubility and oral bioavailability of Avanafil (AVA), a recently approved second generation type 5 phospodiesterase inhibitor used for erectile dysfunction.AVA was formulated as self-nanoemulsifying drug delivery system (SNEDDS) utilizing various oils, surfactants, and cosurfactants. The solubility of AVA in various oils, surfactants, and cosurfactants was determined. Ternary phase diagram was constructed to identify stable nanoemulsion region. The prepared AVA loaded SNEDDS were assessed for optical clarity, droplet size, conductivity, and stability studies.
In vitro
drug release and
in vivo
pharmacokinetic parameters using animal model were also investigated. Results revealed that stable AVA (SNEDDS) were successfully developed with a droplet size range of 65 to 190 nm. SNEDDS composed of 25% dill oil, 55% Tween 80, and 20% propylene glycol successfully improved solubilization of AVA (over 80% within 30 min) vis-a-vis the powder AVA (35% within 30 min).
In vivo
pharmacokinetic showed a significant (
P
< 0.05) increase in C
max
, reduction in T
max
, and SNEDDS enhanced the bioavailability in the rats by 1.4-fold when compared with pure drug.</abstract><cop>Boston</cop><pub>Springer US</pub><pmid>25168449</pmid><doi>10.1208/s12249-014-0199-3</doi><tpages>6</tpages><oa>free_for_read</oa></addata></record> |
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| subjects | Administration, Oral Animals Biochemistry Biological Availability Biomedical and Life Sciences Biomedicine Biotechnology Diffusion Drug Compounding - methods Drug Stability Emulsifying Agents - chemistry Emulsions Male Metabolic Clearance Rate Nanocapsules - administration & dosage Nanocapsules - chemistry Nanocapsules - ultrastructure Particle Size Pharmacology/Toxicology Pharmacy Phase Transition Pyrimidines - administration & dosage Pyrimidines - blood Pyrimidines - chemistry Pyrimidines - pharmacokinetics Rats Rats, Wistar Research Article |
| title | Development and Evaluation of Avanafil Self-nanoemulsifying Drug Delivery System with Rapid Onset of Action and Enhanced Bioavailability |
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