Hollow Multilayer Microcapsules for pH‐/Thermally Responsive Drug Delivery using Aliphatic Poly(urethane‐amine) as Smart Component

Hollow multilayer microcapsules made of aliphatic poly(urethane‐amine) (PUA) and sodium poly(styrene sulfonate) (PSS), templated on PSS‐doped CaCO₃ particles, are prepared for pH‐/thermally responsive drug delivery. The electrostatic interaction and hydrogen bonding under weak‐acid conditions between aliphatic PUA and PSS contribute to the formation of multilayer microcapsules. Scanning electron microscopy (SEM) results demonstrate an obvious variation of the hollow multilayer microcapsules in response to changes in temperature and pH value. Drug‐release behaviors using DOX as a model drug demonstrate that the drug release increases on decreasing the pH value because of the interaction weakness between aliphatic PUA and PSS in acidic conditions. Moreover, the drug release is higher at 55 °C than that at 37 °C for the sake of the shrinkage of aliphatic PUA above its lower critical solution temperature (LCST).

     

Polypeptide/Doxorubicin Hydrochloride Polymersomes Prepared Through Organic Solvent‐free Technique as a Smart Drug Delivery Platform

Rapid and efficient side‐chain functionalization of polypeptide with neighboring carboxylgroups is achieved via the combination of ring‐opening polymerization and subsequent thiol‐yne click chemistry. The spontaneous formation of polymersomes with uniform size is found to occur in aqueous medium via electrostatic interaction between the anionic polypeptide and cationic doxorubicin hydrochloride (DOX·HCl). The polymersomes are taken up by A549 cells via endocytosis, with a slightly lower cytotoxicity compared with free DOX ·HCl. Moreover, the drug‐loaded polymersomes exhibit the enhanced therapeutic efficacy, increase apoptosis in tumor tissues, and reduce systemic toxicity in nude mice bearing A549 lung cancer xenograft, in comparison with free DOX ·HCl.     

Alginate‐Based Microcapsules with a Molecule Recognition Linker and Photosensitizer for the Combined Cancer Treatment

A reactive template method was used to fabricate alginate‐based hydrogel microcapsules. The uniform and well‐dispersed hydrogel capsules have a high drug loading capacity. After they are coated by a folate‐linked lipid mixture on the surface, the capsules possess higher cell uptake efficiency by the molecule recognition between folate and the folate‐receptor overexpressed by the cancer cells. Moreover, in this bioconjugate, the lipid could remarkably reduce the release rate of hydrophilic doxorubicin from the hydrogel microcapsules and encapsulate the hydrophobic photosensitizer hypocrellin B. The biointerfaced capsules could be used as drug carriers for combined treatment against cancer cell proliferation in vitro; this was much more effective than chemotherapy or photodynamic therapy alone.     

Synthesis of Cholesterylated Thiogalactosides for Gene Delivery

A series of cholesterylated thiogalactosides L₁ –L₆ the cell targeting ligands for gene delivery to hepatocytes, was synthesized. Related poly(ethylene glycol) chain was used as a bridge for the attachment of galactoside on one hydroxyl end, while the other hydroxyl end was linked with cholesterol. This design provided an effective entry for the synthesis of a poly(ethylene glycol) compound with the hepatocyte targeting.     

Human Calcitonin Delivered Orally by Means of Nanoparticles Composed of Novel Graft Copolymers

Abstract

The ability of nanoparticles having surface hydrophilic polymeric chains to enhance the oral absorption of human calcitonin was examined in rats. The oral relative bioavailability of calcitonin against its subcutaneous administration was 0.01% without nanoparticles, but increased significantly when it was administered with nanoparticles. Nanoparticles having cationic poly(vinylamine) (PVAm) chains on their surfaces had a relatively stronger enhancing effect than did other nanoparticles. When divinylbenzene was added to the nanoparticle preparation, PVAm nanoparticles with a crosslinked hydrophobic polystyrene core were synthesized. The addition of divinylbenzene resulted in nanoparticles with larger zeta potential through the efficient accumulation of hydrophilic PVAm chains on their surfaces; however, inadequate amounts decreased the zeta potential. Changes in the bioavailability proportional to the zeta potential indicated that the cationic moiety is indispensable for inducing the significant enhancement of calcitonin absorption. The chemical structure of nanoparticles could be optimized by introducing nonionic poly(N‐isopropylacrylamide) (PNIPAAm) or anionic poly(methacrylic acid) chains onto the PVAm nanoparticle surface to effectively further improve the absorption‐enhancing function of PVAm nanoparticles. Finally, the maximum bioavailability of 1.1% was achieved after oral administration of calcitonin with PVAm–PNIPAAm nanoparticles whose components, VAm macromonomer, N‐isopropylacrylamine (NIPAAm) macromonomer, and styrene were copolymerized in the molar ratio of 1.5:0.5:10.     

Atomic Force Microscopy,Transmission Electron Microscopy,and Photon Correlation Spectroscopy: Three Techniques for Rapid Characterization of Optimized Self-Nanoemulsiying Drug Delivery System of Glibenclamide,Carvedilol, and Lovastatin

This article looks at atomic force microscopy as an important aid to characterize the self-nanoemulsifying formulation of glibenclamide, lovastatin, and carvedilol in conjunction with other sophisticated technique, viz., transmission electron microscopy and photon correlation spectroscopy. Sizes obtained by processing the atomic force microscopy (AFM) image are comparable with those obtained from transmission electron microscope. Although in the present study, the mean particle size obtained from photon correlation spectroscopy does not correlate to the findings of atomic force microscopy and transmission electron microscopy, but the poly-disperse index values correlate well with the findings of AFM and transmission electron microscopy where uniform particle size was observed in aqueous dispersion of self-nanoemulsifying formulation of glibenclamide, lovastatin, and carvedilol.     

Structural Transitions of Self-Nanoemulsifying Drug Delivery System of Glibenclamide,Carvedilol, and Lovastatin upon Progressive Aqueous Dilution

The dynamics of morphological transition in amphiphillic systems such as self-nanoemulsifying drug delivery system (SNEDDS) has become an increasingly active field of research in colloidal science. The present contribution deals with the morphological transition of selected optimized SNEDDS formulations of glibenclamide, carvedilol, and lovastatin on progressive aqueous dilution using transmission electron microscopy. The study emphasizes the structural aspects of the systems and stresses the effect of aqueous dilution under which the systems transform from water-in-oil (L₂) phase into bicontinuous structure and, finally, in oil-in-water (L₁) nanodroplets.     

Hydrophobic Derivatives of Dextran Polysaccharide: Characterization and Properties

This study reports the synthesis and characterization of hydrophobic derivatives of dextran in which long alkyl chains substituted a proportion of the hydroxyl groups. These derivatives were characterized by ¹³C and ¹H NMR and infrared spectroscopy. Information about hydrophobic associations in aqueous solutions was obtained by fluorescence spectroscopy in the presence of pyrene and nabumetone probes. These results, in addition to the swelling‐index data of derivatives, showed that there are perspectives of using them as a starting point for models of drug delivery.