Osteoporosis targeting by transdermal distribution has drawn a lot of attention as a cutting-edge, environmentally friendly platform for sustainable pain management. We investigate a novel biocompatible transdermal gel (RCNGL) containing biodegradable chitosan nanoparticles and Risedronate (RS) to treat osteoporosis. The RCNGL was formulated using the Pluronic F 127 co-polymer system and the ionic gelation process. The formulation showed a robust architecture of nanoparticle dispersion with a nano-size range of 201.8 nm when it was thoroughly analysed for Scanning Electron Microscopy, Dynamic electron Microscopy and transmission electron microscopy. At various temperatures, the entrapment efficiency was 67.53±1.05% with steady rheology and respectable porosity, validating FT-IR spectra that showed structural compatibility of RS with other excipients. The drug release test resulted in an 88% RS gel release, supporting sustained release kinetics. The ex vivo Franz diffusion study and in vitro cell uptake and distribution experiments revealed clear cell uptake and distribution with notable skin permeation displaying >70% RS release in mouse epidermal tissue. Overall, our research shows that biodegradable RCNGL may offer a potential osteoporosis and pain control strategy in clinical platforms using passive targeting.
Osteoporosis means "Porous bone” is a disease characterized by progressive bone thinning. The deterioration of bone tissue can lead to bone fragility and fracture, especially of the hip, spine, shoulder and wrist. Osteoporosis is characterized by decreasing bone mineral density (BMD). Bisphosphonates are the most commonly prescribed drugs for the treatment of osteoporosis in the US and many other countries including India. Alendronate (Aln) is a widely used anti-osteoporosis drug, exhibits strong inhibitory effect on bone resorption performed by osteoclast cells. Alendronate-sodium is a BCS class III bisphosphonate, used in the treatment of osteoporosis, acts as a potent, specific inhibitor of osteoclast-mediated bone resorption. Alendronate was the first bisphosphonate to be approved for osteoporosis in the US in 1995. The objective of the present study is to develop, optimize, and evaluate Alendronate-loaded chitosan nanoparticles (NPs) for the treatment of osteoporosis. NPs were prepared by the Ionic gelation method and optimized for various parameters. The prepared nanoparticles were characterized using particle size analyser (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM) and fourier-transform infrared spectroscopy (FTIR). Formulated NPs were obtained in the average size ranging from 60 nm to 220 nm in TEM, SEM and DLS studies. The release profile was depended on the dissolution medium. The proposed nanoparticles offer an interesting alternative for alendronate delivery via the oral route. Our results indicated that alendronate-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.
Osteoporosis is a bone disease caused due to the reducing bone mineral density. Porous and more fragile bones increase the risk of fractures. Hip, spine, shoulder, and wrist bones are commonly affected by osteoporosis. Low bone density is a leading cause of osteoporosis. The most efficient prescribed drugs for the treatment of osteoporosis are bisphosphonates drugs. Alendronate was the first FDA approved bisphosphonate drug for the treatment of osteoporosis. Osteoclast cells are the primary targeting site for alendronate, responsible for bone resorption. A biopharmaceutical classification system class III bisphosphonate acts as a potent, efficient, and bone resorption inhibitor drug. In the present study, alendronate functionalized PLGA based nanoparticles were developed by a solvent diffusion method and optimized for different process variables. The formulated nanoparticles were characterized for surface morphology, particle size distribution, surface charge and drug-polymer compatibility. The scanning electron microscopy and transmission electron microscopy results showed nanoparticle size in the range below 200 nm. The average particle size and zeta potential of the formulated nanoparticles were found to be 175.3 nm and -13.98 mV, respectively. The highest encapsulation efficiency was 65.23%. The release profile was dissolution medium dependent and followed by the Higuchi model of release kinetics.
Osteoporosis means "Porous bone” is a disease characterized by progressive bone thinning. The deterioration of bone tissue can lead to bone fragility and fracture, especially of the hip, spine, shoulder and wrist. Osteoporosis is caused generally due the decreasing bone mineral density (BMD). Osteoporosis affects 30-40% women after menopause all around the world. Bisphosphonates are the most commonly prescribed drugs for the treatment of osteoporosis in the US and many other countries including India. Alendronate- sodium (AS) is a widely used anti-osteoporosis drug, exhibits strong inhibitory effect on bone resorption performed by osteoclast cells and acts as a potent, specific inhibitor of osteoclast-mediated bone resorption. AS was the first FDA approved bisphosphonate for treatment of osteoporosis in the US in 1995. The objective of the present study was to develop, optimize, and evaluate Solid Lipid Nanoparticles (SLN) of Alendronate-sodium drug which improve the solubility, dissolution rate and enhance the bioavailability of the drug. AS loaded Solid Lipid Nanoparticles have been developed using Glyceral Monosterate (GMS) as lipid and poloxamer 407 as the emulsifier by Emulsion -Solvent evaporation method. Different process variables i.e. concentration of surfactant, homogenization speed and time have been optimized. Formulated SLNs with GMS showed low particle size and high entrapement efficiency. The SLNs were characterized using Zeta sizer, transmission electron microscopy (TEM) and scanning electron microscopy (SEM). In-vitro drug release study was performed by dialysis bag diffusion method and different mathematical models were applied for the release study.
In present works we synthesized Donepezil loaded PLGA nanoparticles (NPs). The approach of our research group was to prove the improvement of drug transport through the Blood Brain Barrier when donepezil was loaded with PLGA. It promoted the uptake of drug into brain endothelium compared with the free drug and play a significant role in the treatment of Alzheimer’s disease (AD). The NPs were synthesized by modified Nano precipitation method. These synthesized polymeric nanoparticles were characterized for particle size, Polydispersity index (PDI) and Zeta potential. The average size and PDI of drug loaded polymeric nanoparticle for preferred formulation were found to be 40.8 nm and 0.188 respectively. The Entrapment Efficiency was 74% and Process yield was 78%. The electron microscopic images of polymeric nanoparticles suggested that the particles were spherical in shape. The pharmacokinetics showed that the release behavior of NPs were very much similar to sustained release and follow Hixson Crowell model.
Plasmodium falciparum is one of the most common resistant Plasmodium species responsible for high rates of morbidity and mortality in malaria patients. Clinical guidelines for the management of Plasmodium falciparum include the use of a dose of primaquine phosphate resulting intolerable side effects. Therefore, the aim of this work was to formulate primaquine phosphate-loaded PLGA nanoparticles by using a nanoprecipitation method in order to increase its bioavailability to minimize drug intake. This leads to reduced toxicity and better therapeutic efficacy of the drug. The synthesized nanoparticles were characterized by using dynamic light scattering (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), atomic force microscopy (AFM), Fourier transformed infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD). TEM analysis revealed the presence of smooth spherical-shaped nanoparticles. The drug DLS analysis confirmed the presence of negatively charged nanoparticles with particle size in the range of 100-400 nm. The drug release study was performed to analyses different kinetic models like zero-order model, first-order model, Higuchi model, Hixson-Crowell model, and Korsmeyer-Peppas model.
Objective: The objective of the present study was to develop, optimize, and evaluate Ibandronate-sodium loaded chitosan nanoparticles (Ib-CS NPs) to treat osteoporosis. Methods: NPs were prepared by the Ionic gelation method and optimized for various parameters such as the effect of concentration of chitosan, sodium tripolyphosphate (TPP), and pH effect on particle size polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using particle size analyzer (DLS), transmission electron microscopy (TEM), scanning electron microscopy (SEM), and Fourier-Transform Infrared spectroscopy (FTIR). Results: Formulated NPs were obtained in the average nano size in the range below 200 nm in TEM, SEM, and DLS studies. The particle size and encapsulation efficiency of the optimized formulation were 176.1 nm and 63.28%, respectively. The release profile of NPs was depended on the dissolution medium and followed the First-order release kinetics. Conclusion: Bisphosphonates are the most commonly prescribed drugs for treating osteoporosis in the US and many other countries, including India. Ibandronate is a widely used anti-osteoporosis drug, exhibits a strong inhibitory effect on bone resorption performed by osteoclast cells. Our results indicated that Ibandronate sodium-loaded chitosan nanoparticles provide an effective medication for the treatment of osteoporosis.