Balancing loading, cellular uptake, and toxicity of gelatin‐pluronic nanocomposite for drug delivery: Influence of HLB of pluronic

Abstract

In this study, pluronic stabilized gelatin nanocomposite of varying hydrophilic-lipophilic balance (HLB) were synthesized to study the effect of surface hydrophobicity on their cellular uptake and in turn the delivery of a model hydrophobic bioactive compound, curcumin (CUR). Notably, the variation in HLB from 22 to 8 did not cause much change in morphology (~spherical) and surface charge (~À6.5 mV) while marginally reducing the size of nanocomposite from 165 ± 097 nm to 134 ± 074 nm. On contrary, nanocomposites exhibited a very significant increase in their numbers, hydrophobicity as well as CUR loading with decreasing HLB values (22-8) of pluronic. Further, the cellular uptake of CUR through pluronic-gelatin nanocomposites was studied in human lung carcinoma (A549) cells. The results indicated that cellular uptake of CUR through nanocomposites followed the order HLB 22 > HLB 18 > HLB 15 > HLB 8. This was also reflected in terms of the decrease in cytotoxicity of CUR through nanocomposite of HLB 8 as compared to that of HLB 22. Interestingly, bare nanocomposite of HLB 8 showed significantly higher cytotoxicity as compared to that of HLB 22. Together these results suggested that although higher hydrophobicity of the gelatin-pluronic nanocomposite facilitated higher entrapment of CUR, the carrier per se became toxic due to its hydrophobic interaction with lipid bilayer of plasma membrane. Thus, HLB parameter is very important in designing hybrid nanocomposite systems involving protein and pluronic to ensure both bio-compatibility of the carrier and the optimum cellular delivery of the pay load.

Formulation of Nanomicelles Loaded with Cannabidiol as a Platform for Neuroprotective Therapy

“…Both the small size of the micelles and the surface-active properties of the carriers are a prerequisite for efficient intracellular uptake [32]. The values of zeta-potential were slightly negative, which confirmed previous observations for Pluronic-based micelles [33,34].…”

Mesoporous Silica Particles Functionalized with Newly Extracted Fish Oil (Omeg@Silica) Reducing IL-8 Counteract Cell Migration in NSCLC Cell Lines

“…It is well known that the hydrophilic–lipophilic balance (HLB) of cancer cell membranes is altered, with an increase in cell permeability and enhanced hydrophilic character. Hence, for example, the uptake of hydrophobic curcumin microencapsulated by A549 cells is highest for submicron pluronic-stabilized gelatin particles with the lowest hydrophobicity [ 29 ]. We make the hypothesis that the cellular uptake of both hydrophobic PUFA molecules in triglyceride form (and vitamin D 3 ) [ 30 ] of AnchoisOil, encapsulated and stabilized in the inner porosity of the highly hydrophilic mesoporous silica via endocytosis and direct translocation [ 31 ], is significantly enhanced when compared to the free hydrophobic molecules in the hydrophilic cellular medium.…”

Polymeric micelles as a strategy to enhance the phototoxic efficacy of phenazine photosensitizers

“…The ratio of both components is known as the hydrophilic–lipophilic balance (HLB) of surfactant agents and is related to the ability to interact with different drugs. F‐108 is a more hydrophilic compound than P‐123, presenting HLB values equal to 27 and 8, respectively 23,24 . The use of polymers with a higher hydrophilic or lipophilic character will allow obtaining micelles with dissimilar characteristics in order to select the best delivery system for NR and NRBr.…”

“…F-108 is a more hydrophilic compound than P-123, presenting HLB values equal to 27 and 8, respectively. 23,24 The use of polymers with a higher hydrophilic or lipophilic character will allow obtaining micelles with dissimilar characteristics in order to select the best delivery system for NR and NRBr.…”