Transport of stavudine, delavirdine, and saquinavir across the blood–brain barrier by polybutylcyanoacrylate, methylmethacrylate-sulfopropylmethacrylate, and solid lipid nanoparticles

Polymeric Nanoparticles for Enhancing Antiretroviral Drug Therapy

“…This is due to the tight endothelial cell junctions of the brain capillaries and the presence of efflux transporters such as P-glycoprotein, expressed on the capillary endothelial cell surface (Vauthier et al 2003). Nanoparticulate systems have been identified as an effective carrier for enhancing drug concentration in the brain since they may gain entry by means of endocytosis/phagocytosis and are then shuttled closer to the center of the cell where the drug load is released away from the vicinity of the efflux pumps (Vauthier et al 2003;Kuo and Su 2007). To this end, Kuo (2005) initially reported the loading of stavudine (D4T) into polybutylcyanoacrylate (PBCA) and methylmethacrylate-sulfopropylmethacrylate (MMA-SPM) nanoparticles prepared by emulsion polymerization and free radical polymerization, respectively, for brain targeting.…”

“…The enhanced permeability was attributed to temporary unfolding of right junctions among BMECs upon treatment with alcohol. In a subsequent paper, these authors studied the transport of stavudine (D4T), delaviridine (DLV), and Saquinavir (SQV) across the in vitro BBB using (PBCA), (MMA-SPM), and also solid lipid nanoparticles (SLNs) (Kuo and Su 2007). The results revealed that the permeability of all three drugs increased about 12-16-fold on PBCA, 3-7-fold on MMA-SPM, and 4-11-fold in SLN.…”

“…Permeability coefficient of drugs across HBMEC monolayer by the drug-PBCA complex. (Key) circles for D4T using Y 1 axis; triangles for DLV using Y 2 axis; and squares for SQV using Y 2 axis (Kuo and Su 2007). drugs across the Human brain microvascular endothelial cells (HBMEC) monolayer when encapsulated in PBCA nanoparticles. The higher permeability coefficients with smaller particle size were attributed to the small mass-transfer resistance, hence making it easier to penetrate through the BMEC monolayer as compared with the larger particles.…”

Role of lipid-based excipients and their composition on the bioavailability of antiretroviral self-emulsifying formulations

“…A range of novel strategies are currently being developed for efficient delivery of antiretroviral drugs. Several delivery systems have been reported for the delivery of ARV drugs including bioadhesive coated matrix tablets (Betagiri et al, 2001;Govender et al, 2005), ceramic implants (Benghuzzi, 2000), liposomes Makabi-Panzu et al, 1998;Jin et al, 2005;Ramana et al, 2010), solid colloidal nanoparticles (Kuo & Su, 2007;Chattopadhyay et al, 2008;Kaur et al, 2008;Mainardes et al, 2009), microparticles by supercritical antisolvent method (Sanganwar et al, 2010), dendrimers (Dutta et al, 2007), micelles & microemulsion (Griffin & Driscoll, 2006), nanopowders (Erdenburgh et al, 2007) and suspensions/nanosuspension (Kinman et al, 2003;Yang et al, 2011).…”

Efficacy of intravenous amphotericin B-polybutylcyanoacrylate nanoparticles against cryptococcal meningitis in mice

“…[8][9][10][11] Compared with some other carriers, PBCA was confirmed to ameliorate BBB permeability by 3-to 16-fold. 12 Kreuter and Gelperina 9 used PBCA to transport doxorubicin and found that it significantly increased the survival times of rats with cerebral cancer, leading to complete tumor remission in 20%-40% of the animals. The use of nanoparticles also considerably reduced the effective dosage of doxorubicin, which is limited due to its testicular toxicity and cardiotoxicity.…”