Liposome Transport of Hydrophobic Drugs: Gel Phase Lipid Bilayer Permeability and Partitioning of the Lactone Form of a Hydrophobic Camptothecin, DB‐67

Permeability of Fluid-Phase Phospholipid Bilayers: Assessment and Useful Correlations for Permeability Screening and Other Applications

“…1. The bilayer permeability coefficient is given by the well-known resistances-in-series formula 16,25,26,32,34,35,41,59,62,79,80,83,84 …”

“…35,79,83 In this equation as written, any interfacial resistances 26,32,34,59,62,85 would be represented formally by small values of K lip/w local (>)D lip ⊥,local (>) in thin interfacial zones near ξ = − lip /2 and ξ = lip /2. Broadly speaking, a substantial body of experimental and theoretical work by Xiang, Anderson, and coworkers 26,29,[31][32][33]35,86 and other groups 79,80 suggests that the ordered chain zones (numbered as (2) above) are very often the main barriers to permeation in the liquid crystalline state, that is, rate-limiting for many (one might loosely and cautiously say the "majority" of) permeants, although exceptions exist (see, e.g., Marrink and Bendersen's 80 Fig.…”

“…4 and discussion of oxygen). If the combined length of both these zones on either side of the less ordered core is denoted by barrier , and if they are strongly rate-limiting, then to good approximation 26,29,[32][33][34][35]39,50,62 …”

Evaluation of the cytotoxic effect of camptothecin solid lipid nanoparticles on MCF7 cells

“…This form of CPT expresses higher binding affinity to human serum albumin than the lactone form (Burke et al, 1993), shifting the equilibrium of the drug to the inactive form. However, this inactive form of CPT is not internalized into the cancer cells since the hydroxylactone ring is necessary for a complete reaction with the target for the topoisomerase I (Joguparthi et al, 2008).…”

Biodegradable containers composed of anionic liposomes and cationic polypeptide vesicles

“…[1][2][3] The unique structure of liposomes allows encapsulation of both hydrophilic and hydrophobic compounds, [4][5][6] and liposomes with surface vectortargeting moieties on their surfaces show preferable binding to target cells.…”