Design and Evaluation of New Gel-Based Floating Matrix Tablets Utilizing the Sublimation Technique for Gastroretentive Drug Delivery.

A gel-based floating matrix tablet was formulated and evaluated using the sublimation technique to enhance gastroretentive drug delivery. Anhydrous theophylline was employed as the active pharmaceutical ingredient, combined with sublimation agents and hydroxypropyl methylcellulose as the gel-forming polymer. The resulting tablets exhibited high porosity, immediate floatation, and sustained buoyancy for over 8 h.

Size Reduction Efficiency of Alpha-Mangostin Suspension Using High-Pressure Homogenization.

In this study, we aimed to investigate the effects of stabilizers and processing parameters on the size reduction of alpha-mangostin (AMG) using high-pressure homogenization (HPH). The solubility of AMG in various stabilizers was studied. Selected stabilizers were used to prepare AMG suspensions by HPH under different conditions.

Thermoresponsive Bacteriophage Nanocarrier as a Gene Delivery Vector Targeted to the Gastrointestinal Tract.

The use of the gastrointestinal tract as a site for the local delivery of DNA is an exciting prospect. In order to obtain an effective vector capable of delivering a gene of interest to target cells to achieve sufficient and sustained transgene expression, with minimal toxicity, we developed a new generation of filamentous bacteriophage. This particular bacteriophage was genetically engineered to display an arginine-glycine-aspartic acid (RGD) motif (an integrin-binding peptide) on the major coat protein pVIII and carry a mammalian DNA cassette.

Controllable encapsulation of α-mangostin with quaternized β-cyclodextrin grafted chitosan using high shear mixing.

In this study, the inclusion complex formation between α-mangostin and water-soluble quaternized β-CD grafted-chitosan (QCD-g-CS) was investigated. Inclusion complex formation with encapsulation efficiency (%EE) of 5, 15 and 75% can be varied using high speed homogenizer. Tuning %EE plays a role on physicochemical and biological properties of α-mangostin/QCD-g-CS complex.

Stabilizing ability of surfactant on physicochemical properties of drug nanoparticles generated from solid dispersions.

This study was aimed to examine the nanoparticle formation from redispersion of binary and ternary solid dispersions. Binary systems are composed of various ratios of glibenclamide (GBM) and polyvinylpyrrolidone K30 (PVP-K30), whereas a constant amount at 2.5%w/w of a surfactant, sodium lauryl sulfate (SLS) or Gelucire44/14 (GLC), was added to create ternary systems.

Preparation of fenofibrate dry emulsion and dry suspension using octenyl succinic anhydride starch as emulsifying agent and solid carrier.

Purpose of this study was to investigate the ability of octenyl succinic anhydride (OSA) starch as emulsifier and solid carrier in dry emulsion (DE) and dry suspension (DS) formulations. Fenofibrate (FF) was loaded at lower and higher than its saturation concentration in oil phase to prepare the DE and DS by spray drying method. The DE and DS were successfully prepared with 36-48% and 46% production yield, respectively.

A comparison of eugenol and menthol on encapsulation characteristics with water-soluble quaternized β-cyclodextrin grafted chitosan.

Two guest molecules (eugenol and (-)-menthol) were investigated on inclusion complex formation with water-soluble quaternized β-CD grafted with chitosan (QCD-g-CS). The inclusion complexes were prepared at varying mole ratios between eugenol or (-)-menthol and β-CD (substituted on QCD-g-CS) by a conventional shaking method and obtained as solid powder by freeze-drying process. The results showed that encapsulation efficiency %EE decreased with increasing of initial eugenol or (-)-menthol loading whereas %loading increased with increasing of initial eugenol or (-)-menthol loading.

Lysozyme-magnesium aluminum silicate microparticles: Molecular interaction, bioactivity and release studies.

The objectives of this study were to investigate the adsorption behavior of lysozyme (LSZ) onto magnesium aluminum silicate (MAS) at various pHs and to characterize the LSZ-MAS microparticles obtained from the molecular interaction between LSZ and MAS. The results showed that LSZ could be bound onto the MAS layers at different pHs, leading to the formation of LSZ-MAS microparticles. The higher preparation pH permitted greater adsorption affinity but a lower adsorption capacity of LSZ onto MAS.

Layer-by-layer engineered nanocapsules of curcumin with improved cell activity.

Nanocarriers based on electrostatic Layer-by-layer (LbL) assembly of CaCO3 nanoparticles (CaCO3 NPs) was investigated. These inorganic nanoparticles was used as templates to construct nanocapsules made from films based on two oppositely charged polyelectrolytes, poly(diallyldimethylammonium chloride), and poly (sodium 4-styrene-sulfonate sodium salt), followed by core dissolution. The naked CaCO3 NPs, CaCO3 NPs coated with the polyelectrolytes and hollow nanocapsules were found with hexagonal shape with average sizes of 350-400 nm.

Enhanced permeability across Caco-2 cell monolayers by specific mannosylating ligand of buserelin acetate proliposomes.

Context: Oral delivery of peptide and protein drugs still remains the area of challenges due to their low stability and permeability across GI tract. Among numerous attempts, the receptor-mediated drug targeting is a promising approach to enhance GI permeability.

Objective: The aim of this study was to prepare mannosylated buserelin acetate (MANS-BA) proliposome powders grafted with N-octadecyl-d-mannopyranosylamine (SAMAN) as targeting moiety and evaluate their permeability across Caco-2 cell monolayers.

Surface modification of PLGA nanoparticles by carbopol to enhance mucoadhesion and cell internalization.

Mucoadhesive poly (lactic-co-glycolic acid) (PLGA) nanoparticles having a modified shell-matrix derived from polyvinyl alcohol (PVA) and Carbopol (CP), a biodegradable polymer coating, to improve the adhesion and cell transfection properties were developed. The optimum formulations utilized a CP concentration in the range of 0.05-0.

New metastable form of glibenclamide prepared by redispersion from ternary solid dispersions containing polyvinylpyrrolidone-K30 and sodium lauryl sulfate.

Modification of polymorphic forms of poorly water-soluble drugs is one way to achieve the desirable properties. In this study, glibenclamide (GBM) particles with different polymorphic forms, including a new metastable form, were obtained from redispersion of ternary solid dispersion systems. The ternary solid dispersion systems, consisting of GBM, polyvinylpyrrolidone-K30 (PVP-K30) and sodium lauryl sulfate (SLS), were prepared by solvent evaporation method and subsequently redispersed in deionized water.

Synthesis and anticervical cancer activity of novel pH responsive micelles for oral curcumin delivery.

Curcumin (CM) has demonstrated safety and efficacy as a drug, but its pharmaceutical role is restricted as a result of extremely low aqueous solubility, rapid systemic elimination, inadequate tissue absorption and degradation at alkaline pH; properties that severely curtail its bioavailability. To address this issue, CM was encapsulated within pH responsive amphiphilic chitosan, resulting in the formation of 100 nm spontaneously self-assembled polymeric micelles in water. The amphiphilic chitosan, namely N-benzyl-N,O-succinyl chitosan (BSCS), was prepared by reductive N-benzylation and N,O-succinylation.

Synthesis and fluorescence properties of N-substituted 1-cyanobenz[f]isoindole chitosan polymers and nanoparticles for live cell imaging.

Highly fluorescent N-substituted 1-cyanobenz[f]isoindole chitosans (CBI-CSs) with various degrees of N-substitution (DS) were synthesized by reacting chitosan (CS) with naphthalene-2,3-dicarboxaldehyde (NDA) in the presence of cyanide under mild acidic conditions. Introduction of 1-cyanobenz[f]isoindole moieties into the CS backbone resulted in lowering of polymer thermal stability and crystallinity. The fluorescence quantum yield (Φf) of CBI-CS was found to be DS- and molecular-weight-dependent, with Φf decreasing as DS and molecular weight were increased.

Impact of anti-tacking agents on properties of gas-entrapped membrane and effervescent floating tablets.

Tackiness caused by the gas-entrapped membrane (Eudragit(®)RL 30D) was usually observed during storage of the effervescent floating tablets, leading to failure in floatation and sustained release. In this work, common anti-tacking agents (glyceryl monostearate (GMS) and talc) were used to solve this tackiness problem. The impact of anti-tacking agent on the properties of free films and corresponding floating tablets was investigated.

The effect of surfactant composition on the chemical and structural properties of nanostructured lipid carriers.

Fine-tuning the nanoscale structure and morphology of nanostructured lipid carriers (NLCs) is central to improving drug loading and stability of the particles. The role of surfactant charge on controlling the structure, the physicochemical properties and the stability of NLCs has been investigated using three surfactant types (cationic, anionic, non-ionic), and mixed surfactants. Either one, a mixture of two, or a mixture of three surfactants were used to coat the NLCs, with these classified as one, two and three surfactant systems, respectively.

Effect of N-pyridinium positions of quaternized chitosan on transfection efficiency in gene delivery system.

Methylated N-pyridylmethyl chitosan chlorides (M-PyMeChCs) with a similar total degree of quaternization (DQT) and molecular weight but different N-pyridinium positions were synthesized by reductive amination and methylation, respectively. The effect of N-pyridinium positions on transfection efficiency and cytotoxicity was investigated in human hepatoma (Huh7) cell lines. The results revealed that M-PyMeChCs are able to form a complete complex formation with DNA since there is an N/P ratio of 5.

Application of multiple stepwise spinning disk processing for the synthesis of poly(methyl acrylates) coated chitosan-diclofenac sodium nanoparticles for colonic drug delivery.

The production of pharmaceutical nanoparticles by the spinning disk processing (SDP) technique has advantages in terms of its scalability and its capacity to produce readily tunable nanoparticles of narrow size distribution. In this study, we successfully developed a novel multiple stepwise SDP technique to develop aggregates of uniformly sized poly(methyl acrylates)-coated chitosan-diclofenac sodium nanocores (CS-PMA NPs) for colonic drug delivery. The processing conditions were optimized using the Box-Behnken design.

Nicotine-magnesium aluminum silicate microparticle surface modified with chitosan for mucosal delivery.

Magnesium aluminum silicate (MAS), a negatively charged clay, and nicotine (NCT), a basic drug, can interact electrostatically to form microparticles. Chitosan (CS) was used for the surface modification of the microparticles, and a lyophilization method was used to preserve the original particle morphology. The microparticles were characterized in terms of their physicochemical properties, NCT content, mucoadhesive properties, and release and permeation across porcine esophageal mucosa.

Characterization of chitosan-magnesium aluminum silicate nanocomposite films for buccal delivery of nicotine.

The objective of this study was to prepare and characterize chitosan-magnesium aluminum silicate (CS-MAS) nanocomposite films as a buccal delivery system for nicotine (NCT). The effects of the CS-MAS ratio on the physicochemical properties, release and permeation, as well as on the mucoadhesive properties, were investigated. Molecular interactions between the components of the film were also investigated.

A comparison of spacer on water-soluble cyclodextrin grafted chitosan inclusion complex as carrier of eugenol to mucosae.

In this study two types of water-soluble βCD grafted chitosan were synthesized and compared based on similar degree of N-substitution of βCD moiety; QCD23-g-CS contained methylene spacer and QCDCA22-g-CS contained citric acid spacer. The QCD23-g-CS demonstrated greater eugenol (EG) encapsulation efficiency than that of QCDCA22-g-CS. The micelle-like assemblies of QCD23-g-CS led to slower release of EG while it did not observe in case of QCDCA22-g-CS.

Effects of molecular weight and pyridinium moiety on water-soluble chitosan derivatives for mediated gene delivery.

The aim of this study is to investigate the effects of molecular weight, the pyridinium/trimethyl ammonium (Py/Tr) ratio, the nitrogen atoms (N) in the methylated N-(3-pyridylmethyl) chitosan chloride (M3-PyMeChC)/the phosphorus atoms (P) in DNA (N/P) ratio, and the physicochemical properties of nanopolyplexes on transfection efficiency. The water-soluble chitosan derivative, M3-PyMeChC, was used as a non-viral vector to deliver pEGFP-C2 into human hepatoma (Huh7) cell lines. The results revealed that higher molecular weight M3-PyMeChC was able to form complexes completely with DNA at lower N/P ratios than that with lower molecular weights, which led to higher transfection efficiency.

The PEI-introduced CS shell/PMMA core nanoparticle for silencing the expression of E6/E7 oncogenes in human cervical cells.

In this study, we examined the potential of cationic nanoparticle - polyethyleneimine-introduced chitosan shell/poly (methyl methacrylate) core nanoparticles (CS-PEI) for siRNA delivery. Initially, DNA delivery was performed to validate the capability of CS-PEI for gene delivery in the human cervical cancer cell line, SiHa. siRNA delivery were subsequently carried out to evaluate the silencing effect on targeted E6 and E7 oncogenes.

Water-soluble β-cyclodextrin grafted with chitosan and its inclusion complex as a mucoadhesive eugenol carrier.

Inclusion complex between water-soluble βCD-grafted chitosan derivatives (QCD-g-CS) and eugenol (EG) was investigated as a new type of mucoadhesive drug carrier. The QCD-g-CSs were synthesized with various βCD moieties ranging from 5 to 23%. Spontaneous inclusion complex of these derivatives and EG were found and confirmed by FTIR and simulation study.