title: The role of lipid-based drug delivery systems for enhancing solubility of highly selective antiviral agent acyclovir.
abstract: The study aimed to improve the aqueous solubility and dissolution rate of acyclovir (ACV) using self-emulsifying lipid formulations (SEDDS/SMEDDS). ACV was formulated in various SEDDS/SMEDDS using wide ranges of oils (mono-/di-/triglycerides), nonionic surfactants and water-soluble cosolvents with the aid of phase behavior studies. The drug solubility was determined in anhydrous, 10% and 99% diluted formulations. Drug precipitation and release profiles of the SEDDS/SMEDDS were also investigated. The ACV was highly soluble in the formulations containing high concentration of hydrophilic materials. The addition of propylene glycol (PG) significantly enhanced the drug solubility. In addition, with only 1% 0.1 M HCl, the drug solubility improved 10-fold higher without any precipitation. In the dissolution studies, the representative SEDDS/SMEDDS showed superior release profiles (>90% ACV released) than marketed Zovirax® suspension (<26% released). Formulations containing water-soluble cosolvent (e.g. PG), were the most suitable systems for ACV due to the extensive drug solubilization and release profile.
authors.affiliation: a Kayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University , Riyadh , Saudi Arabia.
authors.forename: Mohsin
authors.initials: M
authors.lastname: Kazi
authors.affiliation: a Kayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University , Riyadh , Saudi Arabia.
authors.forename: Khalid A
authors.initials: KA
authors.lastname: Al-Amri
authors.affiliation: a Kayyali Chair for Pharmaceutical Industries, College of Pharmacy, King Saud University , Riyadh , Saudi Arabia.
authors.forename: Fars K
authors.initials: FK
authors.lastname: Alanazi
mesh_terms: D000212:Acyclovir / Q000008:administration & dosage* / Q000737:chemistry; D000998:Antiviral Agents / Q000819:agonists* / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods*; D016503:Drug Delivery Systems; D065546:Drug Liberation; D004655:Emulsions; D005989:Glycerides / Q000737:chemistry*; D012995:Solubility
chemical_list: D000998:Antiviral Agents; D004337:Drug Carriers; D004655:Emulsions; D005989:Glycerides; D000212:Acyclovir
keywords: Acyclovir; dissolution test; drug precipitation; self-emulsifying/microemulsifying drug delivery systems (SEDDS/SMEDDS)