Publications by authors named "Fakhar Ud Din"
Purpose: This study aimed to develop a solid self-nanoemulsifying drug delivery system (SNEDDS) and surface-coated microspheres to improve the oral bioavailability of niclosamide.
Methods: A solubility screening study showed that liquid SNEDDS, prepared using an optimized volume ratio of corn oil, Cremophor RH40, and Tween 80 (20:24:56), formed nanoemulsions with the smallest droplet size. Niclosamide was incorporated into this liquid SNEDDS and spray-dried with calcium silicate to produce solid SNEDDS.
This study aims to develop a thermoresponsive biomaterial system of irinotecan (IRT) and curcumin (CUR) nano-transferosomal gel (IRT-CUR-NTG) for targeting colorectal cancer (CRC). The IRT-CUR-NTs were statistically optimized and loaded into poloxamer-based thermosensitive gel. Transmission electron microscopy (TEM), Differential scanning calorimetry (DSC) and Fourier-transform infrared spectroscopy (FTIR) of the IRT-CUR-NTs were performed, whereas pH, gelation time, gelation temperature, gel and mucoadhesive strength of the IRT-CUR-NTG were investigated.
View Article and Find Full Text PDFDevelopment of paroxetine loaded nanotransferosomal gel for intranasal delivery with enhanced antidepressant activity in rats.
Colloids Surf B Biointerfaces
February 2025
The aim of this study was to develop paroxetine (PXT) loaded nanotransferosomal gel (PXT-NTFG) for intranasal brain delivery. The process involved fabricating PXT-NTFs (paroxetine-loaded nanotransferosomes) through a thin film hydration method and optimizing them based on parameters such as particle size (PS), zeta potential (ZP), polydispersity index (PDI), and entrapment efficiency (EE). The optimized PXT-NTFs exhibited uniform morphology with a PS of 158.
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- Traumatic brain injury (TBI) leads to neurological deficits and oxidative stress, prompting research into the neuroprotective effects of Daidzein, a phytoestrogen.
- In vitro studies with HT-22 cells showed that Daidzein improved cell survival and reduced harmful nitric oxide production, while in vivo tests using three doses of Daidzein demonstrated significant improvements in neurological functions and anxiety behaviors.
- Molecular analysis indicated that Daidzein enhances antioxidant defenses and reduces markers of cell damage and apoptosis, showing promise as a treatment for TBI-related complications.
Article Synopsis
- Fimasartan is a drug with poor solubility, leading to low bioavailability, so researchers developed a fluidized solid dispersion (FFSD) using a fluid bed granulator to enhance its solubility.
- The study found that the FFSD, made with hydroxypropyl methylcellulose (HPMC) and microcrystalline cellulose, increased the dissolution and absorption of fimasartan compared to a commercial tablet.
- Testing in beagle dogs showed that the FFSD tablet had significantly higher plasma concentrations and overall drug availability, suggesting it could be an effective oral formulation for fimasartan.
Herein, we reported novel docetaxel-decorated solid lipid nanoparticle (DCT-SLN)-loaded dual thermoreversible system (DCT-DRTS) for intramuscular administration with reduced burst effect, sustained release and improved antitumor efficacy. The optimized DCT-DRTs was subjected to in-vitro and in-vivo analyses. Antitumor evaluation of the DCT-DRTS was executed and compared with DCT-hydrogel, and DCT-suspension trailed by the histopathological and immune-histochemical analyses.
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- A novel technique was developed to improve the water solubility and oral bioavailability of aceclofenac using different nanoparticle systems, with sodium carboxymethylcellulose (Na-CMC) proving to be the most effective polymer.
- Various methods like spray-drying were used to create different solid dispersions with aceclofenac and Na-CMC, which resulted in nanoparticles with distinct properties such as size and morphology.
- The study found that the self-nanoemulsifying drug delivery system (SNEDDS) had the best overall performance in enhancing drug solubility and bioavailability, making the nanoparticle screening method a valuable tool for improving other poorly soluble compounds.
Letrozole (LTZ) is used as first-line treatment for hormone-positive breast cancer (BC) in postmenopausal women. However, its poor aqueous solubility and permeability have reduced its clinical efficacy. Herein, we developed LTZ-nanotransferosomes (LTZ-NT) to address above mentioned issues.
View Article and Find Full Text PDFThe objective of this study was to develop nanotechnology-mediated paclitaxel (PAC) and curcumin (CUR) co-loaded solid lipid nanoparticles (PAC-CUR-SLNs) for the treatment of lung cancer, which is a leading cause of death worldwide. Around 85 % cases of lungs cancer constitute non-small cell lung cancer (NSCLC). PAC-CUR-SLNs were prepared via high pressure homogenization.
View Article and Find Full Text PDFNeurons and their connecting axons gradually degenerate in neurodegenerative diseases (NDs), leading to dysfunctionality of the neuronal cells and eventually their death. Drug delivery for the treatment of effected nervous system is notoriously complicated because of the presence of natural barriers, i.e.
View Article and Find Full Text PDFPurpose: Anti-leishmanial medications administered by oral and parenteral routes are less effective for treatment of cutaneous leishmaniasis (CL) and cause toxicity, hence targeted drug delivery is an efficient way to improve drug availability for CL with reduced toxicity. This study aimed to develop, characterize and evaluate nitazoxanide and quercetin co-loaded nanotransfersomal gel (NTZ-QUR-NTG) for the treatment of CL.
Methods: NTZ-QUR-NT were prepared by thin film hydration method and were statistically optimized using Box-Behnken design.
The purpose of this study was to investigate the impact of carrier hydrophilicity on solid self nano-emulsifying drug delivery system (SNEDDS) and self nano-emulsifying granule system (SEGS). The mesoporous calcium silicate (Ca-silicate) and hydroxypropyl-β-cyclodextrin (HP-β-CD) were utilised as hydrophobic carrier and hydrophilic carrier, respectively. The liquid SNEDDS formulation, composed of Tween80/Kollipohr EL/corn oil (35/50/15%) with 31% (w/w) dexibuprofen, was spray-dried and fluid-bed granulated together with Avicel using Ca-silicate or HP- β-CD as a solid carrier, producing four different solid SNEDDS and SEGS formulations.
View Article and Find Full Text PDFCardiovascular diseases (CVDs) are considered as the leading cause of death worldwide. CVD continues to be a major cause of death and morbidity despite significant improvements in its detection and treatment. Therefore, it is strategically important to be able to precisely characterize an individual's sensitivity to certain illnesses.
View Article and Find Full Text PDFTacrolimus (TRL) is used for the treatment of atopic dermatitis (AD) due to its T-cell stimulation effect. However, its significantly poor water solubility, low penetration and cytotoxicity have reduced its topical applications. Herein, tacrolimus loaded nano transfersomes (TRL-NTs) were prepared, followed by their incorporation into chitosan gel to prepare tacrolimus loaded nano transfersomal gel (TRL-NTsG).
View Article and Find Full Text PDFRevaprazan (REV), a novel reversible Proton Pump Inhibitor (PPI) used to treat peptic ulcers, faces challenges in therapeutic efficacy due to its poor dissolution properties and a short half-life. Solid lipid nanoparticles (SLNs) have emerged as a drug delivery system capable of enhancing dissolution and bioavailability of lipid soluble drugs. Here, we report on the development and optimization of a smart gastro-retentive raft system of REV-loaded SLNs (GRS/REV-SLNs) to enhance drug bioavailability and gastric retention.
View Article and Find Full Text PDFOsteoporosis (OP), is a systemic bone disorder associated with low bone mass and bone tissue corrosion. Worsening of the disease condition leads to bone delicacy and fracture. Various drugs are available for the treatment of OP, however they have limitations including poor solubility, bioavailability and toxicity.
View Article and Find Full Text PDFThe current study explores the potential of melatonin (MLT)-loaded solid lipid nanoparticles (MLT-SLNs) for better neuroprotective effects in ischemic stroke. MLT-SLNs were prepared using lipid matrix of palmityl alcohol with a mixture of surfactants (Tween 40, Span 40, Myrj 52) for stabilizing the lipid matrix. MLT-SLNs were tested for physical and chemical properties, thermal and polymorphic changes, drug release and neuroprotective studies in rats using permanent middle cerebral artery occlusion (-MCAO) model.
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- Migraine is a neurological condition that can cause nausea and vomiting, and traditional treatments like sumatriptan (SUT) have limitations due to issues with absorption and effectiveness.
- Researchers developed a new delivery method using SUT loaded nano-ethosomes (SUT-NEs) combined with a chitosan-based mucoadhesive gel (SUT-NEsG) for intranasal application, enhancing drug properties and efficacy.
- Studies showed that SUT-NEsG improves drug absorption in the brain and effectiveness in migraine models, indicating it could be a promising treatment option compared to standard oral doses.
Honokiol is a phytochemical component with a variety of pharmacological properties. However, the major limitation of Honokiol is its poor solubility and low oral bioavailability. In this study, we formulated and characterized oral Honokiol-loaded solid lipid nanoparticles (SLNs) to enhance bioavailability and then evaluated their effectiveness in experimental diabetic neuropathy (DN).
View Article and Find Full Text PDFHerein we designed, optimized, and characterized the Metformin Hydrochloride Transethosomes (MTF-TES) and incorporate them into Chitosan gel to develop Metformin Hydrochloride loaded Transethosomal gel (MTF-TES gel) that provides a sustained release, improved transdermal flux and improved antidiabetic response of MTF. Design Expert® software (Ver. 12, Stat-Ease, USA) was applied for the statistical optimization of MTF-TES.
View Article and Find Full Text PDFObjectives: Rivaroxaban (RXB), a novel Xa inhibitor having groundbreaking therapeutic potential. However, this drug is associated with few limitations, including its pharmacokinetics related toxicities. Here, we developed RXB-loaded SLNs (RXB-SLNs) to improve its biopharmaceutical profile.
View Article and Find Full Text PDFVincristine (VCR) is a well-known chemotherapeutic agent that frequently triggers neuropathic pain. Ajugarin-I (Aju-I) isolated from Ajuga bracteosa exerts antioxidant, anti-inflammatory, and neuroprotective properties. The present study was designed to investigate the ameliorative potential of Aju-I against VCR-induced neuropathic pain and explored the underlying mechanism involved.
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