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Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate
Purpose: To enhance the aqueous solubility and dissolution rate of elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles (SLNs) using solvent injection method. Methods: EVG-loaded SLNs were prepared by solvent injection method. Four different formulations of SLN were prepared using...
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| Published in: | Tropical journal of pharmaceutical research 2015-09, Vol.14 (9), p.1549-1556 |
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| Main Authors: | , , |
| Format: | Article |
| Language: | English |
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| container_end_page | 1556 |
| container_issue | 9 |
| container_start_page | 1549 |
| container_title | Tropical journal of pharmaceutical research |
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| creator | Kommavarapu, Pavan Maruthapillai, Arthanareeswari Palanisamy, Kamaraj |
| description | Purpose: To enhance the aqueous solubility and dissolution rate of
elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles
(SLNs) using solvent injection method. Methods: EVG-loaded SLNs were
prepared by solvent injection method. Four different formulations of
SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya
lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous
phase. The SLNs were characterized for various physical properties,
including particle size, zeta potential, polydispersity, release
profile and entrapment efficiency. Results: The yield of SLNs was in
the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes
were observed in mean particle size (nm), Z - potential (mV) and
polydispersity index (PDI) of the SLNs by varying the concentration of
cryoprotectant. EVG - SLNs demonstrated a 800 - 1030-fold
enhancement in aqueous solubility compared with plain EVG. The
dissolution efficiency (DE) for SLNs was > 63 % in all cases and
increased up to 83 % with increasing lipid load. Conclusion: Successful
preparation and characterization of elvitegravir-loaded solid
lipid nanoparticles by solvent injection method has been accomplished
in this study. |
| doi_str_mv | 10.4314/tjpr.v14i9.2 |
| format | article |
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elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles
(SLNs) using solvent injection method. Methods: EVG-loaded SLNs were
prepared by solvent injection method. Four different formulations of
SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya
lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous
phase. The SLNs were characterized for various physical properties,
including particle size, zeta potential, polydispersity, release
profile and entrapment efficiency. Results: The yield of SLNs was in
the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes
were observed in mean particle size (nm), Z - potential (mV) and
polydispersity index (PDI) of the SLNs by varying the concentration of
cryoprotectant. EVG - SLNs demonstrated a 800 - 1030-fold
enhancement in aqueous solubility compared with plain EVG. The
dissolution efficiency (DE) for SLNs was > 63 % in all cases and
increased up to 83 % with increasing lipid load. Conclusion: Successful
preparation and characterization of elvitegravir-loaded solid
lipid nanoparticles by solvent injection method has been accomplished
in this study.</description><identifier>ISSN: 1596-5996</identifier><identifier>EISSN: 1596-9827</identifier><identifier>DOI: 10.4314/tjpr.v14i9.2</identifier><language>eng</language><publisher>Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria</publisher><subject>Cryoprotectant ; Elvitegravir ; Entrapment efficiency ; Lipid load ; Solid lipid nanoparticles</subject><ispartof>Tropical journal of pharmaceutical research, 2015-09, Vol.14 (9), p.1549-1556</ispartof><rights>Copyright 2015 - Tropical Journal of Pharmaceutical Research</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-b312t-f53ebf5dd4d338ff8ed4a6f97232780d03c389627fadde3d52440a4da47eaa993</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,860,27903,27904</link.rule.ids></links><search><creatorcontrib>Kommavarapu, Pavan</creatorcontrib><creatorcontrib>Maruthapillai, Arthanareeswari</creatorcontrib><creatorcontrib>Palanisamy, Kamaraj</creatorcontrib><title>Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate</title><title>Tropical journal of pharmaceutical research</title><description>Purpose: To enhance the aqueous solubility and dissolution rate of
elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles
(SLNs) using solvent injection method. Methods: EVG-loaded SLNs were
prepared by solvent injection method. Four different formulations of
SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya
lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous
phase. The SLNs were characterized for various physical properties,
including particle size, zeta potential, polydispersity, release
profile and entrapment efficiency. Results: The yield of SLNs was in
the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes
were observed in mean particle size (nm), Z - potential (mV) and
polydispersity index (PDI) of the SLNs by varying the concentration of
cryoprotectant. EVG - SLNs demonstrated a 800 - 1030-fold
enhancement in aqueous solubility compared with plain EVG. The
dissolution efficiency (DE) for SLNs was > 63 % in all cases and
increased up to 83 % with increasing lipid load. Conclusion: Successful
preparation and characterization of elvitegravir-loaded solid
lipid nanoparticles by solvent injection method has been accomplished
in this study.</description><subject>Cryoprotectant</subject><subject>Elvitegravir</subject><subject>Entrapment efficiency</subject><subject>Lipid load</subject><subject>Solid lipid nanoparticles</subject><issn>1596-5996</issn><issn>1596-9827</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2015</creationdate><recordtype>article</recordtype><recordid>eNpFkNlKxDAUhoMoOI7e-QB5gGltli65lLEuUFRcrstpkzgZaluSWBgfwae20w4Kh7P8fPxwfoQuSRRyRviV3_Y2HAg3IqRHaEFikQQio-nxYY-FSE7RmXPbKIoTIcgC_Txb1YMFb7p2hdebca29suZ7UjC0EucDNF_z2WmcN4Px6sPCYGxQdCCVxK9dYyQuTD_2R2i70dCbulEO687ivN1AW8_YV2Ua43eT741xblQm4xfw6hydaGicujjMJXq_zd_W90HxdPewvi6CihHqAx0zVelYSi4Zy7TOlOSQaJFSRtMskhGrWSYSmmqQUjEZU84j4BJ4qgCEYEu0mn1r2zlnlS57az7B7koSlfscy32O5ZRjSUc8nPHKjG-26o-urYHyXxyLxDSi7Bfr_nzf</recordid><startdate>20150901</startdate><enddate>20150901</enddate><creator>Kommavarapu, Pavan</creator><creator>Maruthapillai, Arthanareeswari</creator><creator>Palanisamy, Kamaraj</creator><general>Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria</general><scope>RBI</scope><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>20150901</creationdate><title>Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate</title><author>Kommavarapu, Pavan ; Maruthapillai, Arthanareeswari ; Palanisamy, Kamaraj</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-b312t-f53ebf5dd4d338ff8ed4a6f97232780d03c389627fadde3d52440a4da47eaa993</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2015</creationdate><topic>Cryoprotectant</topic><topic>Elvitegravir</topic><topic>Entrapment efficiency</topic><topic>Lipid load</topic><topic>Solid lipid nanoparticles</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kommavarapu, Pavan</creatorcontrib><creatorcontrib>Maruthapillai, Arthanareeswari</creatorcontrib><creatorcontrib>Palanisamy, Kamaraj</creatorcontrib><collection>Bioline International</collection><collection>CrossRef</collection><jtitle>Tropical journal of pharmaceutical research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kommavarapu, Pavan</au><au>Maruthapillai, Arthanareeswari</au><au>Palanisamy, Kamaraj</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate</atitle><jtitle>Tropical journal of pharmaceutical research</jtitle><date>2015-09-01</date><risdate>2015</risdate><volume>14</volume><issue>9</issue><spage>1549</spage><epage>1556</epage><pages>1549-1556</pages><issn>1596-5996</issn><eissn>1596-9827</eissn><abstract>Purpose: To enhance the aqueous solubility and dissolution rate of
elvitegravir (EVG) by formulating the drug as solid lipid nanoparticles
(SLNs) using solvent injection method. Methods: EVG-loaded SLNs were
prepared by solvent injection method. Four different formulations of
SLN were prepared using gelucire - 44/14 as lipid core in ethanol, soya
lecithin as emulsifier, and polysorbate 80 as surfactant in the aqueous
phase. The SLNs were characterized for various physical properties,
including particle size, zeta potential, polydispersity, release
profile and entrapment efficiency. Results: The yield of SLNs was in
the range 151.0 ± 2.4 to 199.1 ± 2.7 nm. Significant changes
were observed in mean particle size (nm), Z - potential (mV) and
polydispersity index (PDI) of the SLNs by varying the concentration of
cryoprotectant. EVG - SLNs demonstrated a 800 - 1030-fold
enhancement in aqueous solubility compared with plain EVG. The
dissolution efficiency (DE) for SLNs was > 63 % in all cases and
increased up to 83 % with increasing lipid load. Conclusion: Successful
preparation and characterization of elvitegravir-loaded solid
lipid nanoparticles by solvent injection method has been accomplished
in this study.</abstract><pub>Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria</pub><doi>10.4314/tjpr.v14i9.2</doi><tpages>8</tpages><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1596-5996 |
| ispartof | Tropical journal of pharmaceutical research, 2015-09, Vol.14 (9), p.1549-1556 |
| issn | 1596-5996 1596-9827 |
| language | eng |
| recordid | cdi_crossref_primary_10_4314_tjpr_v14i9_2 |
| source | Directory of Open Access Journals |
| subjects | Cryoprotectant Elvitegravir Entrapment efficiency Lipid load Solid lipid nanoparticles |
| title | Preparation, Characterization and Evaluation of Elvitegravir-Loaded Solid Lipid Nanoparticles for Enhanced Solubility and Dissolution Rate |
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