14 research outputs found
Spray drying of fenofibrate loaded nanostructured lipid carriers
AbstractThe conversion of aqueous dispersion of nanostructured lipid carriers (NLCs) into dry powder by spray drying could be a useful approach to render NLCs with better physical chemical stability than the aqueous dispersion. In this study, aqueous NLC dispersion containing fenofibrate was converted into dry, easily reconstitutable powder using spray drying. A central composite face centered design (CCFD) was used to investigate the influence of the ratio of lipid to protectant (mannitol and trehalose) and crystallinity of spray-dried powder on the particle size, yield and residual moisture content of the dried powder. A linear relationship (R2 = 0.9915) was established between the crystalline content of the spray-dried powders against the ratio of mannitol to trehalose from 3:7 to 10:0 (w/w). Spray drying of NLC aqueous dispersion using a mannitol and trehalose mixture resulted in an increase in particle size of the NLCs after reconstitution in water as compared to that in the initial aqueous dispersion. The decrease in crystallinity of the dry powder by reducing the ratio of mannitol to trehalose could improve the reconstitution of the NLCs in water. However the yield and residual moisture content of dry powder decreased with an increase in the ratio of mannitol to trehalose. Lipid nanoparticles were able to retain the drug incorporation and the prolonged drug release profile after spray drying. The experimental model was robust, and suggested that spray drying is a viable technique for the conversion of NLCs into dry powder
Thermosensitive Liposomal Codelivery of HSA–Paclitaxel and HSA–Ellagic Acid Complexes for Enhanced Drug Perfusion and Efficacy Against Pancreatic Cancer
Fibrotic
stroma and tumor-promoting pancreatic stellate cells (PSCs), critical
characters in the pancreatic ductal adenocarcinoma (PDA) microenvironment,
promote a tumor-facilitating environment that simultaneously prevents
drug penetration into tumor foci and stimulates tumor growth. Nab-PTX,
a human serum albumin (HSA) nanoparticle of paclitaxel (PTX), indicates
enhanced matrix penetration in PDA probably due to its small size <i>in vivo</i> and high affinity of HSA with secreted protein acidic
and rich in cysteine (SPARC), overexpressed in the PDA stroma. However,
this HSA nanoparticle shows poor drug blood retention because of its
weak colloidal stability <i>in vivo</i>, thus resulting
in insufficient drug accumulation within tumor. Encapsulating HSA
nanoparticles into the internal aqueous phase of ordinary liposomes
improves their blood retention and the following tumor accumulation,
but the large 200 nm size and shielding of HSA in the interior might
make it difficult for this hybrid nanomedicine to penetrate the fibrotic
PDA matrix and promote bioavailability of the payload. In our current
work, we prepared ∼9 nm HSA complexes with an antitumor drug
(PTX) and an anti-PSC drug (ellagic acid, EA), and these two HSA–drug
complexes were further coencapsulated into thermosensitive liposomes
(TSLs). This nanomedicine was named TSL/HSA-PE. The use of TSL/HSA-PE
could improve drug blood retention, and upon reaching locally heated
tumors, these TSLs can rapidly release their payloads (HSA–drug
complexes) to facilitate their further tumor accumulation and matrix
penetration. With superior tumor accumulation, impressive matrix penetration,
and simultaneous action upon tumor cells and PSCs to disrupt PSCs–PDA
interaction, TSL/HSA-PE treatment combined with heat exhibited strong
tumor growth inhibition and apoptosis <i>in vivo</i>