Olanzapine (OLZ) is classified as a typical antipsychotic drug utilized for the treatment of schizophrenia. Its oral bioavailability is 60% due to its low solubility and pre-systemic metabolism. Hence, the present work aims to formulate and evaluate OLZ nanoparticles dissolving microneedles (MNs) for transdermal delivery to overcome the problems associated with drug administration orally. OLZ nanoparticles were prepared by the nanoprecipitation method. The optimized OLZ nanoparticle formula was utilized for the fabrication of dissolving MNs by loading OLZ nanodispersion into polydimethylsiloxane (PDMS) micromould cavities, followed by casting the polymeric solution of polyvinylpyrrolidone(PVP-K30) and polyvinyl alcohol (PVA) to form MN matrix. The results revealed that the optimized OLZ nanoparticle formula (NP-5) exhibited particle size 115.76±5.45 nm, entrapment efficiency 78.4±5.46, and zeta potential -19.01±1.6 mV. The results of MNs revealed that MN-4 exhibits a high drug content of 98.52%, and ex vivo permeation through rabbit skin exhibited that MN-4 permeates more effectively than a simple patch by approximately 5.16 fold. In vivo pharmacokinetics study revealed that the area under curve AUC 0-∞ of MN-4 was 6054.56±376 ng. h/ml as compared with AUC0-∞ of marketed OLZ tablet was 3975.77±373 ng. h/ml. It can be concluded that the dissolving MN-4 patch is considered a promising formula to overcome the problems associated with drug administration orally and could improve drug bioavailability, in addition to the ease of administering the medication to schizophrenic patients.
Background: Frovatriptan succinate (FVT) is an effective medication used to treat migraines; however, available oral formulations suffer from low permeability; accordingly, several formulations of FVT were prepared. Objective: Prepare, optimize, and evaluate FVT-BE formulation to develop enhanced intranasal binary nano-ethosome gel. Methods: Binary ethosomes were prepared using different concentrations of phospholipid PLH90, ethanol, propylene glycol, and cholesterol by thin film hydration and characterized by particle size, zeta potential, and entrapment efficiency. Furthermore, in-vitro, in-vivo, ex-vivo, pharmacokinetics, and histopathological studies were done. Results: Regarding FVT-loaded BE, formula (F9) demonstrated the best paramet
... Show MoreThe aim of the present study is to formulate, evaluate and characterize the nanoemulsion of Domperidone a poorly water-soluble anti-emetic drug.
Domperidone powder is white or almost white powder, photosensitive, practically insoluble in water, slightly soluble in ethanol and in methanol; soluble in dimethylformamide. It is used as an antiemetic for the short-term treatment of nausea and vomiting of various etiologies.
Solubility studies were conducted to select the oil, surfactant and cosurfactant. Phase diagrams were constructed by aqueous phase
... Show MoreWe report here an innovative feature of green nanotechnology-focused work showing that mangiferin—a glucose functionalized xanthonoid, found in abundance in mango peels—serves dual roles of chemical reduction and in situ encapsulation, to produce gold nanoparticles with optimum in vivo stability and tumor specific characteristics. The interaction of mangiferin with a Au-198 gold precursor affords MGF-198AuNPs as the beta emissions of Au-198 provide unique advantages for tumor therapy while gamma rays are used for the quantitative estimation of gold within the tumors and various organs. The laminin receptor specificity of mangiferin affords specific accumulation of therapeutic payloads of this new therapeutic agent within prostate tumors
... Show MorePiroxicam (PIR) is a nonsteroidal anti-inflammatory drug of oxicam category, used in gout, arthritis, as well as other inflammatory conditions (topically and orally). PIR is practically insoluble in water, therefore the aim is prepare and evaluate piroxicam as liquid self-nanoemulsifying drug delivery system to enhance its dispersibility and stability. The Dispersibilty and Stability study have been conducted in Oil, Surfactant and Co-surfactant for choosing the best materials to dissolve piroxicam. The pseudo ternary phase diagrams have been set at 1:1, 2:1, 3:1 as well as 4:1 ratio of surfactants and co-surfactants, also there are 4 formulations were prepared by using various concentrations of transcutol HP, cremophore EL and triacetin
... Show MoreVisceral leishmaniosis is one of the most fatal old-world neglected disease with estimated 90 thousand worldwide cases emerge each year. In Iraq, the cutaneous and visceral form are endemic but available chemotherapies are either toxic with diverse side effects, expensive available drugs or parasite …
The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTI
... Show MoreTwo groups of chronic hepatitis B and C virus patients were divided into Pre-treated patients (25 CHB patients with positive HBs Ag for more than 6 months and 40 CHC patients), and post-treated patients [12 CHB patients (4, 6, and 2 were treated with lamivudine, IFN-? and combination of LMV + IFN-? respectively), and 27 patients for CHC (3, 13 and 11 patients were treated with Ribavirin, IFN-? and combination therapy (RBV+ IFN-?) respectively].These patients were followed up for 6 months. By using ELISA technique, levels of IL-6, IL-10, IFN-? and TNF-? were measured in vivo and in vitro (supernatant of PBMCs stimulated with PHA) and compared with healthy control. The mean level of IL-6, IL-10 and TNF-? in CHB patients showed significant dif
... Show More1267 Objectives Aim to evaluate 198Au nanoparticles (AuNP) biodistribution and uptake in a human prostate model for treatment. Many phytochemicals are known to have anti-tumor properties but have short half-lives in vivo. We hypothesized that using these phytochemicals to formulate and coat AuNP would inhibit enzyme cleavage and enhance their anti-tumor properties. Initial evaluations were performed in SCID mice bearing PC3 tumors. Methods : 198AuNP were formulated with the following gum Arabic, epigalocatechin gallate (EGCg) pomegranate extract and mangiferin extract. The resultant nanoparticles were evaluated in normal mice and in human prostate bearing SCID mice. The tumor bearing mice were injected intratumorally with 3-5 uCi of 198A
... Show MoreImproved oral bioavailability of lipophilic substances can be achieved using self-emulsifying drug delivery systems. However, because the properties of self-emulsifying are greatly influenced by surfactant amount and type, type of oil used, droplet size, charge, cosolvents, and physiological variables, the synthesis of self-emulsifying is highly complex; consequently, only a small number of excipient self-emulsifying formulations has been developed so far for clinical use. This study reports a highly effective procedure for developing self-emulsifying formulations using a novel approach based on the hydrophilic-lipophilic difference theory. Microemulsion characteristics, such as the constituents and amounts of oil and surfactant electrolyte
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