Naproxen-Gelucire Nanoformulations for Improved Solubility and Dissolution Rate of Poorly Water-Soluble Drug Naproxen

Abstract

Naproxen-Gelucire Nanoformulations (NFs) in terms of their phase solubility behavior, physico-chemical characteristics, cytotoxicity and morphology and dissolution enhancement has been studied using the poorly water soluble drug, naproxen. The NFs were prepared via wet milling using a conventional Retsch Planetary ball mill in various ratios of drug to polymer (1:1, 1:2, 1:3, 1:4). The release rate of naproxen from various ratios of drug/polymer nanoparticles was investigated using USP paddle apparatus (type II). A comparative phase solubility of naproxen was performed in different carrier concentrations of simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The highest dissolution enhancement was achieved for the formulation with ratio of 1:4. This is a 160% enhancement when compared to that of the pure drug. The ability of amphiphillic surfactant carriers to accelerate in vitro dissolution of poorly water-soluble drugs has been attributed to wetting, micellar solubilization, and/or deflocculation. The Korsemeyer-Peppas model most aptly fits the in vitro dissolution data and gives an insight into the possible drug release mechanisms predominated by anamolous non-Fickian diffusion. Thus, the nanoformulations studied can help improve the physicochemical characteristics of naproxen towards its dissolution enhancement and possibly will increase the oral bioavailability of the drug without any adverse cytotoxic consequences.

Nanoplatforms of Manganese Ferrite Nanoparticles Functionalized with Anti‐Inflammatory Drugs

“…the physicochemical characteristics, brain penetration properties and dosage of the drugs. Conventional analgesic NSAIDs include acetylsalicylic acid (ASA), mefenamic acid (MEF), and naproxen (NAP) , . NSAIDs are widely administered against a wide range of inflammatory diseases to treat moderate pain including fever, headache, dental pain, postoperative and postpartum pain, dysmenorrhea, osteoarthritis, rheumatoid arthritis .…”

“…Conventional analgesic NSAIDs include acetylsalicylic acid (ASA), mefenamic acid (MEF), and naproxen (NAP) , . NSAIDs are widely administered against a wide range of inflammatory diseases to treat moderate pain including fever, headache, dental pain, postoperative and postpartum pain, dysmenorrhea, osteoarthritis, rheumatoid arthritis . However, NSAIDs are accompanied with limitations such as lack of specificity toward desired tissues, high distribution volume, lack of selectivity, poor aqueous solubility and dissolution rate.…”

“…Nonetheless, appropriate functionalization of the MNPs could result in the design of multifunctional drug carriers, finding applications as contrast agents in magnetic resonance imaging and/or in magnetic hyperthermia , . Even though polymeric nanoparticles and MNPs have been studied in the area of theranostics in the sense that diagnosis coexists with targeted drug and/or gene delivery in case of tumors, the use of MNPs as NSAIDs carriers has been scarcely reported …”

Fabrication of Celecoxib PVP Microparticles Stabilized by Gelucire 48/16 via Electrospraying for Enhanced Anti-Inflammatory Action

“…Additionally, the coexistence of hydrophilic carriers like Gelurice ® 48/16 may decrease the hydrophobicity of the drug particle surfaces, which will subsequently increase interaction with the aqueous medium and boost the rate of CXB’s dissolution [ 7 ]. Several previous studies showed the enhanced release performance exhibited after the addition of Gelurice ® 48/16 [ 27 , 28 , 29 ].…”