A Review on Commercial Oligonucleotide Drug Products.

Oligonucleotide drug products commercially approved in the US and the EU are reviewed. A total of 20 products that includes 1 aptamer, 12 antisense oligonucleotides (ASOs), 6 small interfering ribonucleic acids (siRNAs), and 1 mixture of single-stranded and double-stranded polydeoxyribonucleotides have been identified. A typical oligonucleotide formulation is composed of an oligonucleotide with buffering agent(s), pH adjusting agents, and a tonicity adjusting agent.

Current State of Minitablet Product Design: A Review.

Interest in minitablets (MTs) has grown exponentially over the last 20 years and especially the last decade, as evidenced by the number of publications cited in Scopus and PubMed. MTs offer significant opportunities for personalized medicine, dose titration and flexible dosing, taste masking, and customizing drug delivery systems. Advances in specialized MT tooling, manufacturing, and characterization instrumentation have overcome many of the earlier development issues.

Predictive Performance Comparison of Computed Linear and Quadratic Multivariate Models for In-Situ UV Fiber Optics Tablet Dissolution Testing.

A present investigation aimed for multivariate modeling as a solution to resolve inaccuracy in dissolution testing experienced in the use of in-situ UV fiber optics dissolution systems (FODS) due to signal saturation problems. This problem is specifically encountered with high absorbance of moderate to high dose formulations. A high absorbance not only impede a real-time assessment but can also result in inaccurate dissolution profiles.

Formulation and optimization of sildenafil citrate-loaded PLGA large porous microparticles using spray freeze-drying technique: A factorial design and in-vivo pharmacokinetic study.

The oral administration of sildenafil citrate (SC) for the treatment of pulmonary arterial hypertension is associated with several drawbacks. The study aimed to design and formulate SC-loaded inhalable poly (lactic-co-glycolic acid) [PLGA] large porous microparticles (LPMs) for pulmonary delivery. A factorial design was used to study the effect of the composition of LPMs on physicochemical properties.

Self-Assembling PCL-PAMAM Linear Dendritic Block Copolymers (LDBCs) for Bioimaging and Phototherapeutic Applications.

This study represents a successful approach toward employing polycaprolactone-polyamidoamine (PCL-PAMAM) linear dendritic block copolymer (LDBC) nanoparticles as small-molecule carriers in NIR imaging and photothermal therapy. A feasible and robust synthetic strategy was used to synthesize a library of amphiphilic LDBCs with well-controlled hydrophobic-to-hydrophilic weight ratios. Systems with a hydrophobic weight ratio higher than 70% formed nanoparticles in aqueous media, which show hydrodynamic diameters of 51.

Computational Predictability of Microsponge Properties Using Different Multivariate Models.

The capabilities of principal component regression (PCR) and multiple linear regression (MLR) were evaluated to decipher and predict the impact of formulation and process parameters on the modeled metronidazole benzoate (MB)-ethyl cellulose (EC) microsponge (MBECM) properties. MBECM were prepared by a quasi-emulsion solvent diffusion method. A minimum experimentation was designed using Box-Behnken approach with one center point after initial screening experiments.

Design and evaluation of novel inhalable sildenafil citrate spray-dried microparticles for pulmonary arterial hypertension.

Pulmonary delivery of vasodilators is a promising alternative for the intravenous and oral treatment of pulmonary arterial hypertension (PAH). The aim of this study was to design and evaluate hydrogel microparticles as a carrier for sustained pulmonary delivery of sildenafil citrate. Spray dried hydrogel microparticles containing biodegradable sodium carboxymethyl cellulose, sodium alginate, and sodium hyaluronate polymers at variable concentrations were prepared.

Physical properties and solubility studies of Nifedipine-PEG 1450/HPMCAS-HF solid dispersions.

Low-order high-energy nifedipine (NIF) solid dispersions (SDs) were generated by melt solvent amorphization with polyethylene glycol (PEG) 1450 and hypromellose acetate succinate (HPMCAS-HF) to increase NIF solubility while achieving acceptable physical stability. HPMCAS-HF was used as a crystallization inhibitor. Individual formulation components, their physical mixtures (PMs), and SDs were characterized by differential scanning calorimetry, powder X-ray diffraction, and Fourier transform infrared spectroscopy (FTIR).

Deciphering magnesium stearate thermotropic behavior.

Magnesium stearate (MgSt) is the most commonly used excipient for oral solid dosage forms, yet there is significant commercial physicochemical variability that can lead to variable performance of critical product attributes. Differential scanning calorimetry (DSC) is often used as a quality control tool to characterize MgSt, but little data is available regarding the physicochemical relevance for the DSC thermograms. The main aim of this study was to decipher MgSt's complex thermotropic behavior using DSC, thermogravimetric analysis, capillary melting point, polarized hot-stage microscopy, and temperature dependent small-angle X-ray scattering (SAXS) and assign physicochemical relevance to the DSC thermograms.

Dipalmitoylphosphatidylcholine (DPPC): Annealing Strategy to Mitigate Variability in Thermotropic and Moisture Sorption Behavior.

Dipalmitoylphosphatidylcholine (DPPC) demonstrated complex differential scanning calorimetry (DSC) thermal behavior. Transitions below 100°C showed variability in their thermotropic reversibility. An experimental design employing a DSC heat-cool-heat-cool-heat cycle and modulated DSC were used to gain insight into the DPPC's complex thermal nature.

Inhalable Ipratropium Bromide Particle Engineering with Multicriteria Optimization.

Spray-dried ipratropium bromide (IPB) microspheres for oral inhalation were engineered using Quality by Design. The interrogation of material properties, process parameters, and critical product quality attributes interplay enabled rational product design. A 2 screening design exhibited the Maillard reaction between L-leucine (LL) and lactose at studied outlet temperatures (OT) >130°C.