Multilayered polymer coating modulates mucoadhesive and biological properties of camptothecin-loaded lipid nanocapsules.

Lipid core nanocapsules (NCs) coated with multiple polymer layers were rationally designed as a potential approach for the colonic delivery of camptothecin (CPT). Chitosan (CS), hyaluronic acid (HA) and hypromellose phthalate (HP) were selected as coating materials, to modulate the mucoadhesive and permeability properties of CPT regarding the improvement of local and targeted action in the colon cancer cells. NCs were prepared by emulsification/solvent evaporation method and coated with multiple polymer layers by polyelectrolyte complexation technique.

Supersaturating drug delivery systems containing fixed-dose combination of two antihypertensive drugs: Formulation, in vitro evaluation and molecular metadynamics simulations.

The purpose of this study was to associate the poorly water-soluble antihypertensive drugs candesartan cilexetil (CC) and hydrochlorothiazide (HCTZ) as fixed-dose combination, in the form of ternary Amorphous Solid Dispersions (ASD), using hydroxypropylmethylcellulose acetate succinate (HPMCAS) type M as polymeric carrier. The potential of the system to generate and to maintain supersaturation of both drugs was also evaluated. The ASDs were prepared by ball milling technique and solid-state characterization was performed by differential scanning calorimetry (DSC), Fourier transformed infrared spectroscopy (FTIR) and X-ray powder diffraction (XRPD).

Understanding the interaction between Soluplus® and biorelevant media components.

Soluplus® (polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer) is a solubilizing copolymer commonly applied as carrier in solid dispersions of poorly soluble drugs. This polymer is used to increase the apparent solubility of drugs with low aqueous solubility and consequently enhance drug absorption by the human gastrointestinal tract. To select the appropriate carrier to compose solid dispersions, in vitro supersaturation studies were applied as a pre-formulation tool, using different dissolution media.

New supersaturating drug delivery system as strategy to improve apparent solubility of candesartan cilexetil in biorelevant medium.

Candesartan cilexetil (CC) is a poorly soluble antihypertensive drug with absorption limited by its low aqueous solubility. Aiming to generate CC supersaturation as strategy to improve its absorption and bioavailability, amorphous solid dispersions (ASDs) of CC with hydroxypropylmethylcellulose acetate succinate type M (HPMCAS M) were developed and evaluated by and techniques. The ASDs were characterized by several solid-state techniques and evaluated regarding the supersaturation generation and maintenance under conditions in biorelevant medium.

HPMCAS as an effective precipitation inhibitor in amorphous solid dispersions of the poorly soluble drug candesartan cilexetil.

Among the strategies to improve the biopharmaceutic properties of poorly soluble drugs, Supersaturating Drug Delivery Systems like polymer-based amorphous solid dispersions (SD) have been successfully applied. The screening of appropriate polymeric carriers to compose SD is a crucial point on their development. In this study, hydroxypropylmethylcellulose (HPMC), hydroxypropylmethylcellulose acetate succinate (HPMCAS) types L, M and H and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer (SOL) were evaluated by in vitro supersaturation studies regarding their anti-precipitant ability on the poorly soluble drug candesartan cilexetil (CC) under two different media, including biorelevant conditions.