Synthesis of N-vinylpyrrolidone/Acrylic acid nanoparticles for drug delivery: Method optimization

There are various approaches to deliver therapeutic agents to the preferred target. Polymeric nanoparticles were found to have pleasing suitability as a drug carrier. The goal of this research was to optimize the synthesis method to obtain the desirable %yield and particle properties of the new biocompatible polymer-based nanoparticles. The non-toxic polymer, N-vinyl pyrrolidone (NVP) and a widely used hydrophilic biocompatible acrylic acid (AA) monomer were used to form the drug nanocarriers. The synthesis method was optimized by changing the types of initiator (KPS or V50) and the monomers molar ratio (NVP:AA). It was found that by varying both the monomer molar ratio and the type of reaction initiator, did not have significant effect on the physicochemical characteristics of the nanocarriers. The FTIR spectra of all products exhibited the peaks of carboxylic acid, carbonyl, and tertiary amine functional group vibration. The particle size of the nanocarriers was in the range of 173.6 ± 18.4 to 201.4 ± 17.1 nm with negative surface charge. However, the yield obtained increased as the initiator was altered from KPS to V50, and when the acrylic acid molar ratio was increased from 1:1 to 1:3. In conclusion, changing the initiator and monomer molar ratio may affect the physicochemical properties of the nanocarriers and the %yield of the nanocarrier product. Further investigations are essential to obtain the favorable drug nanocarriers for drug delivery

Synthesis of Polyethylene Glycol Diacrylate/Acrylic Acid Nanoparticles as Nanocarriers for the Controlled Delivery of Doxorubicin to Colorectal Cancer Cells

Doxorubicin (Dox) is known for its potential to deliver desirable anticancer effects against various types of cancer including colorectal cancer. However, the adverse effects are serious. This study aimed to synthesize polyethylene glycol diacrylate (PEGDA)/acrylic acid (AA)-based nanoparticles (PEGDA/AA NPs) for Dox delivery to colorectal cancer cells. The NPs were synthesized using free-radical polymerization reaction using the monomers PEGDA and AA with their physical properties, drug loading and release, biocompatibility, and anticancer effect evaluated. The NPs were spherical with a size of around 230 nm, with a 48% Dox loading efficiency and with loading capacity of 150 µg/mg. Intriguingly, the NPs had the ability to prolong the release of Dox in vitro over 24 h and were non-toxic to intestinal epithelial cells. Dox-loaded PEGDA/AA NPs (Dox-NPs) were able to effectively kill the colorectal cancer cell line (HT-29) with the Dox-NPs accumulating inside the cell and killing the cell through the apoptosis pathway. Overall, the synthesized PEGDA/AA NPs exhibit considerable potential as a drug delivery carrier for colon cancer-directed, staged-release therapy

Development and Optimization of <i>Andrographis paniculata</i> Extract-Loaded Self-Microemulsifying Drug Delivery System Using Experimental Design Model

The objectives of this study were to develop an optimized formulation for an Andrographis paniculata extract (AGPE)-loaded self-microemulsifying drug delivery system (SMEDDS) using an experimental design and evaluate the characteristics of the developed SMEDDS. The solubility of andrographolide (AGP) in various solvents was investigated. The pseudo-ternary phase was constructed to provide an optimal range for each component to form microemulsions (MEs). The formulation was optimized using an I-optimal design mixture type, where the physical stability, droplet size, polydispersity index, and zeta potential were examined. Soft capsules of the optimized AGPE-loaded SMEDDS were manufactured. The dissolution and ex vivo membrane permeation were studied. Oleic acid, Tween® 80, and PEG 400 were the best solubilizers for AGP. The promising surfactant to co-surfactant ratio to generate ME was 3:1. The optimized SMEDDS contained 68.998% Tween® 80, with 13.257% oleic acid and 17.745% PEG 400. The assayed content of AGP, uniformity of dosage unit, and stability complied with the expected specifications. The dissolution and membrane permeability of AGPE-loaded SMEDDS was significantly improved from the A. paniculata extract (p < 0.05). All in all, the developed optimized AGPE-loaded SMEDDS was proven to contain optimal composition and AGP content where a stable ME could spontaneously be formed with enhanced delivery efficacy

In Vitro Biological Activity and In Vivo Human Study of Porcine-Placenta-Extract-Loaded Nanovesicle Formulations for Skin and Hair Rejuvenation

Porcine placenta extract (PPE) contains many water-soluble macromolecular compounds, such as proteins and growth factors, which have limited transportation through the skin. This study aimed to assess the effect of porcine-placenta-extract (PPE)-loaded nano-transdermal systems for skin repair and hair growth promotion. The potentials of the nanoformulation for cytotoxicity, cell proliferation, intracellular reactive oxygen species (ROS) reduction, lipoxygenase inhibition, intracellular inflammatory cytokine reduction, and cell aggregation were evaluated. PPE-entrapped niosome nanovesicles were produced by thin-film hydration and probe-sonication methods, followed by incorporation in a skin serum formulation. The physicochemical properties of the formulation were examined, and the efficacy of the serum formulation was elucidated in humans. The results showed that PPE had no toxicity and was able to induce cell growth and cell aggregation. In addition, PPE significantly decreased intracellular ROS, inhibited lipoxygenase activity, and reduced the production of intracellular tumor necrosis factor-α. In the in vivo human study, the PPE nanovesicles-loaded serum could improve skin properties by increasing skin hydration. Moreover, it was capable of promoting hair growth by increasing hair elongation and melanin index after application for one month. Consequently, the PPE nanovesicles-loaded serum was effective for skin anti-aging and hair rejuvenation

Synthesis of

There are various approaches to deliver therapeutic agents to the preferred target. Polymeric nanoparticles were found to have pleasing suitability as a drug carrier. The goal of this research was to optimize the synthesis method to obtain the desirable %yield and particle properties of the new biocompatible polymer-based nanoparticles. The non-toxic polymer, N-vinyl pyrrolidone (NVP) and a widely used hydrophilic biocompatible acrylic acid (AA) monomer were used to form the drug nanocarriers. The synthesis method was optimized by changing the types of initiator (KPS or V50) and the monomers molar ratio (NVP:AA). It was found that by varying both the monomer molar ratio and the type of reaction initiator, did not have significant effect on the physicochemical characteristics of the nanocarriers. The FTIR spectra of all products exhibited the peaks of carboxylic acid, carbonyl, and tertiary amine functional group vibration. The particle size of the nanocarriers was in the range of 173.6 ± 18.4 to 201.4 ± 17.1 nm with negative surface charge. However, the yield obtained increased as the initiator was altered from KPS to V50, and when the acrylic acid molar ratio was increased from 1:1 to 1:3. In conclusion, changing the initiator and monomer molar ratio may affect the physicochemical properties of the nanocarriers and the %yield of the nanocarrier product. Further investigations are essential to obtain the favorable drug nanocarriers for drug delivery

Facile, sensitive and reagent-saving smartphone-based digital image colorimetric assay of captopril tablets enabled by long-pathlength RGB acquisition

A new assay of captopril (CTP) tablets was developed based on digital image colorimetry using Ellman’s reagent. For the first time, a facile technique of increasing the analytical path was applied in this work to enhance the sensitivity. For this purpose, the reaction solutions were photographed using a smartphone while they were contained in two 1-cm pathlength cuvettes which were placed side by side. The Red-Green-Blue (RGB) in term of [B/(R+G+B)] was used to plot a standard curve. Compared to using a single cuvette, double cuvettes resulted in more precise analytical signals and better linearity (r2 of 0.9992). Additionally, CTP could be analyzed at low concentrations (2.5–25 µM) with LOD of 0.70 µM and LOQ of 2.13 µM, thus lowering the reagent consumption. The assay was proven to be valid, and it was greener, faster, and more affordable than the pharmacopeial chromatographic method, thereby suitable for pharmaceutical quality control

Maleimide-functionalized carboxymethyl cellulose: A novel mucoadhesive polymer for transmucosal drug delivery

The objective of this research was to develop a novel mucoadhesive polymer for drug delivery applications based on N-(2-aminoethyl) maleimide-functionalized carboxymethyl cellulose in which the weight ratios of the materials were tuned to explore the condition providing the highest maleimide content on the polymer. The polymers were synthesized from N-(2-aminoethyl) maleimide that was conjugated to carboxymethyl cellulose with their mucoadhesive properties examined by tensile testing, rheology, and flow-through analysis and their biocompatibilities evaluated on the human gingival fibroblast cell line (HGF-1). The anti-inflammatory drug benzydamine was loaded into mucoadhesive-polymer-based tablets and used to demonstrate the application of the synthesized polymer. The polymer exhibited superior mucoadhesive capability compared to carboxymethyl cellulose through the interaction between maleimide moiety and mucin. The functionalized polymer also possessed the ability to control the release of benzydamine with Higuchi's release model and was proven to be a potential candidate in mucoadhesive drug delivery