Improvement of physicochemical parameters of acyclovir using cocrystallization approach
ABSTRACT Acyclovir is an antiviral drug having potent activity against the virus of herpes family and varicella zoster. Unfortunately, drug suffers very poor oral bioavailability (15-30%). The main objective of present study was to develop acyclovir cocrystals with improved solubility which may resu...
| Main Authors: | , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Universidade de São Paulo
|
| Series: | Brazilian Journal of Pharmaceutical Sciences |
| Subjects: | |
| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400727&lng=en&tlng=en |
| _version_ | 1818568761238618112 |
|---|---|
| author | Jignasa Ketan Savjani Chirag Pathak |
| author_facet | Jignasa Ketan Savjani Chirag Pathak |
| author_sort | Jignasa Ketan Savjani |
| collection | DOAJ |
| description | ABSTRACT Acyclovir is an antiviral drug having potent activity against the virus of herpes family and varicella zoster. Unfortunately, drug suffers very poor oral bioavailability (15-30%). The main objective of present study was to develop acyclovir cocrystals with improved solubility which may result in improvement of bioavailability. Hansen solubility approach was used as a tool to predict the cocrystal formation of a drug with selected coformer. Cocrystals of acyclovir with various coformers were screened in order to enhance their water solubility. Cocrystals of the drug were prepared using various methods like solvent evaporation, wet grinding, and antisolvent addition. Formation of cocrystals by solvent evaporation method was found to be better method amongst all. Optimization of cocrystal formation was carried out by employing different solvents as well as the stoichiometric ratio of acyclovir with that of coformer. Synthesis of cocrystals was optimized using water as a solvent system resulted in good agreements. The potential cocrystal formation of acyclovir was characterized by IR, PXRD and DSC techniques. An in-vitro dissolution study was performed to determine the dissolution rate of cocrystals. The results suggest that acyclovir forms cocrystals with tartaric acid and the initial dissolution rate of synthesized cocrystals were considerably faster as compared to pure acyclovir. |
| first_indexed | 2024-12-14T06:39:21Z |
| format | Article |
| id | doaj.art-9e136367f8554af6b3ef4ca655804181 |
| institution | Directory Open Access Journal |
| issn | 2175-9790 |
| language | English |
| last_indexed | 2024-12-14T06:39:21Z |
| publisher | Universidade de São Paulo |
| record_format | Article |
| series | Brazilian Journal of Pharmaceutical Sciences |
| spelling | doaj.art-9e136367f8554af6b3ef4ca6558041812022-12-21T23:13:17ZengUniversidade de São PauloBrazilian Journal of Pharmaceutical Sciences2175-979052472773410.1590/s1984-82502016000400017S1984-82502016000400727Improvement of physicochemical parameters of acyclovir using cocrystallization approachJignasa Ketan SavjaniChirag PathakABSTRACT Acyclovir is an antiviral drug having potent activity against the virus of herpes family and varicella zoster. Unfortunately, drug suffers very poor oral bioavailability (15-30%). The main objective of present study was to develop acyclovir cocrystals with improved solubility which may result in improvement of bioavailability. Hansen solubility approach was used as a tool to predict the cocrystal formation of a drug with selected coformer. Cocrystals of acyclovir with various coformers were screened in order to enhance their water solubility. Cocrystals of the drug were prepared using various methods like solvent evaporation, wet grinding, and antisolvent addition. Formation of cocrystals by solvent evaporation method was found to be better method amongst all. Optimization of cocrystal formation was carried out by employing different solvents as well as the stoichiometric ratio of acyclovir with that of coformer. Synthesis of cocrystals was optimized using water as a solvent system resulted in good agreements. The potential cocrystal formation of acyclovir was characterized by IR, PXRD and DSC techniques. An in-vitro dissolution study was performed to determine the dissolution rate of cocrystals. The results suggest that acyclovir forms cocrystals with tartaric acid and the initial dissolution rate of synthesized cocrystals were considerably faster as compared to pure acyclovir.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400727&lng=en&tlng=enAcyclovir/studyAcyclovir/dissolution studyCocrystal/techniqueHansen solubility parametersSolvent evaporation method. |
| spellingShingle | Jignasa Ketan Savjani Chirag Pathak Improvement of physicochemical parameters of acyclovir using cocrystallization approach Brazilian Journal of Pharmaceutical Sciences Acyclovir/study Acyclovir/dissolution study Cocrystal/technique Hansen solubility parameters Solvent evaporation method. |
| title | Improvement of physicochemical parameters of acyclovir using cocrystallization approach |
| title_full | Improvement of physicochemical parameters of acyclovir using cocrystallization approach |
| title_fullStr | Improvement of physicochemical parameters of acyclovir using cocrystallization approach |
| title_full_unstemmed | Improvement of physicochemical parameters of acyclovir using cocrystallization approach |
| title_short | Improvement of physicochemical parameters of acyclovir using cocrystallization approach |
| title_sort | improvement of physicochemical parameters of acyclovir using cocrystallization approach |
| topic | Acyclovir/study Acyclovir/dissolution study Cocrystal/technique Hansen solubility parameters Solvent evaporation method. |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502016000400727&lng=en&tlng=en |
| work_keys_str_mv | AT jignasaketansavjani improvementofphysicochemicalparametersofacyclovirusingcocrystallizationapproach AT chiragpathak improvementofphysicochemicalparametersofacyclovirusingcocrystallizationapproach |