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1.
Am J Trop Med Hyg ; 110(6): 1127-1136, 2024 Jun 05.
Article in English | MEDLINE | ID: mdl-38697074

ABSTRACT

Animal African trypanosomiasis, also known as nagana, is caused by Trypanosoma species, which cause significant clinical diseases and lead to losses in animal production. We carried out a cross-sectional survey to investigate the composition of vectors and parasite diversity in two districts in the eastern region of Ghana where pigs and cattle were exposed to tsetse bites. We performed cytochrome c oxidase subunit 1 polymerase chain reaction (PCR) to identify tsetse species and internal transcribed spacer 1 PCR to identify Trypanosoma species. Also, we investigated the source of tsetse blood meal based on mitochondrial cytochrome b gene sequence analysis. A total of 229 tsetse, 65 pigs, and 20 cattle were investigated for trypanosomes. An overall vector density of 4.3 tsetse/trap/day was observed. A trypanosome prevalence of 58.9% (95% CI = 52.5-65.1%), 46.2% (95% CI = 34.6-58.1%), and 0.0% (95% CI = 0.0-16.1%) in tsetse, pigs, and cattle, respectively, was detected. Trypanosoma congolense was predominant, with a prevalence of 33.3% (95% CI = 73.3-86.5%) in tsetse. There was evidence of multiple infections in tsetse and pigs. Approximately 39% of the tsetse were positive for multiple infections of T. congolense and Trypanosoma simiae. Parasite prevalence in pigs across the communities was high, with significant differences associated between locations (χ2 = 28.06, 95% CI = 0.05-0.81, P = 0.0009). Tsetse blood meal analysis revealed feeding on domestic Sus scrofa domesticus (pigs) and Phacochoerus africanus (warthogs). Infective tsetse may transmit trypanosomes to livestock and humans in the communities studied.


Subject(s)
Trypanosoma , Trypanosomiasis, African , Tsetse Flies , Animals , Ghana/epidemiology , Tsetse Flies/parasitology , Cattle , Trypanosomiasis, African/transmission , Trypanosomiasis, African/epidemiology , Trypanosomiasis, African/veterinary , Swine , Trypanosoma/isolation & purification , Trypanosoma/genetics , Trypanosoma/classification , Cross-Sectional Studies , Swine Diseases/transmission , Swine Diseases/epidemiology , Swine Diseases/parasitology , Insect Vectors/parasitology , Forests , Cattle Diseases/epidemiology , Cattle Diseases/transmission , Cattle Diseases/parasitology , Prevalence , Female
2.
AAPS PharmSciTech ; 24(8): 222, 2023 Nov 07.
Article in English | MEDLINE | ID: mdl-37935931

ABSTRACT

This study reports on the synthesis of Mn1 - xZnxFe2O4 (Mn, Zn ferrite) magnetic nanoparticles (MNPs) as drug delivery carriers for effective therapeutic outcomes. The MNPs were prepared using the coprecipitation method, and their magnetic properties were investigated based on their composition. Among the compositions tested, Mn0.8Zn0.2Fe2O4 MNPs exhibited superparamagnetic properties with a saturation magnetization moment of 34.6 emu/g at room temperature (25°C). To enhance the water solubility of curcumin (Cur), known for its hydrophobic nature, it was successfully loaded onto alginate (Alg)/chitosan (Chit)@Mn0.8Zn0.2Fe2O4 nanoparticles (NPs). The nanocomposite was characterized by field emission scanning electron microscopy (FE-SEM) which revealed a particle size of approximately 20 nm. The crystalline structure of the NPs was analyzed using X-ray diffraction, while Fourier-transform infrared (FTIR), energy-dispersive X-ray, and map analysis techniques were employed for further characterization. In terms of drug release, there was an initial burst release of Cur (around 18%) within the first hour, followed by a slower release (approximately 61%) over the next 36 h. The anti-tumor properties of the Cur-loaded NPs were evaluated using the Methyl Thiazol Tetrazolium (MTT) assay and quantitative real-time polymerase chain reaction. The MTT assay confirmed a higher cytotoxic effect of Cur-loaded Alg/Chit@Mn0.8Zn0.2Fe2O4 NPs on the MCF-7 breast cancer cell line compared to free Cur, highlighting the significance of incorporating Cur into nano-sized carrier systems.


Subject(s)
Breast Neoplasms , Chitosan , Curcumin , Nanoparticles , Humans , Female , Curcumin/pharmacology , Curcumin/chemistry , Chitosan/chemistry , Alginates/chemistry , Breast Neoplasms/drug therapy , Drug Carriers/chemistry , Nanoparticles/chemistry , Zinc , Particle Size
3.
Pharmaceutics ; 15(8)2023 Aug 17.
Article in English | MEDLINE | ID: mdl-37631368

ABSTRACT

Hypromellose, a widely used polymer in the pharmaceutical industry, is available in several grades, depending on the percentage of substitution of the methoxyl and hydroxypropyl groups and molecular weight, and in various functional forms (e.g., suitable for direct compression tableting). These differences can affect their physicomechanical properties, and so this study aims to characterise the particle size and mechanical properties of HPMC K100M polymer grades from four different vendors. Eight polymers (CR and DC grades) were analysed using scanning electron microscopy (SEM) and light microscopy automated image analysis particle characterisation to examine the powder's particle morphology and particle size distribution. Bulk density, tapped density, and true density of the materials were also analysed. Flow was determined using a shear cell tester. Flat-faced polymer compacts were made at five different compression forces and the mechanical properties of the compacts were evaluated to give an indication of the powder's capacity to form a tablet with desirable strength under specific pressures. The results indicated that the CR grades of the polymers displayed a smaller particle size and better mechanical properties compared to the DC grade HPMC K100M polymers. The DC grades, however, had better flow properties than their CR counterparts. The results also suggested some similarities and differences between some of the polymers from the different vendors despite the similarity in substitution level, reminding the user that care and consideration should be given when substitution is required.

4.
Biomedicines ; 11(6)2023 Jun 17.
Article in English | MEDLINE | ID: mdl-37371841

ABSTRACT

Upregulation of cyclooxygenase (COX-2) plays an important role in lung cancer pathogenesis. Celecoxib (CLX), a selective COX-2 inhibitor, may have beneficial effects in COVID-19-induced inflammatory storms. The current study aimed to develop carrier-free inhalable CLX microparticles by electrospraying as a dry powder formulation for inhalation (DPI). CLX microparticles were prepared through an electrospraying method using a suitable solvent mixture at two different drug concentrations. The obtained powders were characterized in terms of their morphology, solid state, dissolution behavior, and aerosolization performance. Electrosprayed particles obtained from the ethanol-acetone solvent mixture with a drug concentration of 3 % w/v exhibited the best in vitro aerosolization properties. The value of the fine particle fraction obtained for the engineered drug particles was 12-fold higher than that of the untreated CLX. When the concentration of CLX was increased, a remarkable reduction in FPF was obtained. The smallest median mass aerodynamic diameter was obtained from the electrosprayed CLX at a 3% concentration (2.82 µm) compared to 5% (3.25 µm) and untreated CLX (4.18 µm). DSC and FTIR experiments showed no change in drug crystallinity or structure of the prepared powders during the electrospraying process. The findings of this study suggest that electrospraying has potential applications in the preparation of DPI formulations.

5.
J Drug Deliv Sci Technol ; 84: 104486, 2023 Jun.
Article in English | MEDLINE | ID: mdl-37123173

ABSTRACT

Inhalation phage therapy is proposed as a replacement approach for antibiotics in the treatment of pulmonary bacterial infections. This study investigates phage therapy on bacterial pneumonia in patients with moderate to severe COVID-19 via the inhalation route. In this double-blind clinical trial, 60 patients with positive COVID-19 hospitalized in three central Mazandaran hospitals were chosen and randomly divided into two intervention and control groups. Standard country protocol drugs plus 10 mL of phage suspension every 12 h with a mesh nebulizer was prescribed for 7 days in the intervention group. The two groups were compared in terms of O2Sat, survival rate, severe secondary pulmonary bacterial infection and duration of hospitalization. Comparing the results between the intervention and control group, in terms of the trend of O2Sat change, negative sputum culture, no fever, no dyspnea, duration of hospitalization, duration of intubation and under ventilation, showed that the difference between these two groups was statistically different (P value < 0.05). In conclusion, inhalation phage therapy may have a potential effect on secondary infection and in the outcome of COVID-19 patients. However, more clinical trials with control confounding factors are needed to further support this concept.

6.
Malar J ; 22(1): 76, 2023 Mar 04.
Article in English | MEDLINE | ID: mdl-36870966

ABSTRACT

BACKGROUND: The World Health Organization recommends parasitological confirmation of all suspected malaria cases by microscopy or rapid diagnostic tests (RDTs) before treatment. These conventional tools are widely used for point-of-care diagnosis in spite of their poor sensitivity at low parasite density. Previous studies in Ghana have compared microscopy and RDT using standard 18S rRNA PCR as reference with varying outcomes. However, how these conventional tools compare with ultrasensitive varATS qPCR has not been studied. This study, therefore, sought to investigate the clinical performance of microscopy and RDT assuming highly sensitive varATS qPCR as gold standard. METHODS: 1040 suspected malaria patients were recruited from two primary health care centers in the Ashanti Region of Ghana and tested for malaria by microscopy, RDT, and varATS qPCR. The sensitivity, specificity, and predictive values were assessed using varATS qPCR as gold standard. RESULTS: Parasite prevalence was 17.5%, 24.5%, and 42.1% by microscopy, RDT, and varATS qPCR respectively. Using varATS qPCR as the standard, RDT was more sensitive (55.7% vs 39.3%), equally specific (98.2% vs 98.3%), and reported higher positive (95.7% vs 94.5%) and negative predictive values (75.3% vs 69.0%) than microscopy. Consequently, RDT recorded better diagnostic agreement (kappa = 0.571) with varATS qPCR than microscopy (kappa = 0.409) for clinical detection of malaria. CONCLUSIONS: RDT outperformed microscopy for the diagnosis of Plasmodium falciparum malaria in the study. However, both tests missed over 40% of infections that were detected by varATS qPCR. Novel tools are needed to ensure prompt diagnosis of all clinical malaria cases.


Subject(s)
Malaria, Falciparum , Malaria , Humans , Microscopy , Polymerase Chain Reaction , Ghana
7.
Int J Pharm ; 631: 122507, 2023 Jan 25.
Article in English | MEDLINE | ID: mdl-36535457

ABSTRACT

In this study, the Supercritical Carbon Dioxide (scCO2) gas foaming procedure was used in the preparation of scaffolds containing the model drug dexamethasone (DXMT). The method used did not include an organic solvent thus making it a safe method. The ring-opening polymerization of PCL-PEG-PCL (PCEC) triblock was conducted using an organocatalyst [1,8 diazabicyclo [5.4.0] undec-7-ene (DBU)]. After mixing 5.0 g of DXMT with 50.0 g of PCEC, hydraulic pressure was applied to compress the mixed powder into disc-like tablets. The tablet-like scaffold of the triblock containing DXMT was inserted into a scCO2 gas-foaming device. The peak porosity percentage of the synthesized triblock was found to be 55.58 %. Pressure, temperature, soaking time and the time required to depressurize were recorded as 198 bar, 50 °C, 2.0 h, and 28 min respectively. After treatment with scCO2, the scaffolds experienced an almost full release of DXMT in vitro after 30 days (83.74 ± 1.54 % vs 52.24 ± 2.03 % before scCO2 treatment). In conclusion, the results proved that the scCO2 gas foaming procedure could be employed for constructing modifiable PCEC scaffolds with plausible porosity and structural and morphological features which can manipulate drug release.


Subject(s)
Carbon Dioxide , Tissue Scaffolds , Tissue Scaffolds/chemistry , Carbon Dioxide/chemistry , Porosity , Polyethylene Glycols/chemistry , Polyesters/chemistry , Tissue Engineering/methods
8.
Int J Pharm ; 625: 122099, 2022 Sep 25.
Article in English | MEDLINE | ID: mdl-35961417

ABSTRACT

Cancer is the second cause of human mortality after cardiovascular disease around the globe. Conventional cancer therapies are chemotherapy, radiation, and surgery. In fact, due to the lack of absolute specificity and high drug concentrations, early recognition and treatment of cancer with conventional approaches have become challenging issues in the world. To mitigate against the limitations of conventional cancer chemotherapy, nanomaterials have been developed. Nanomaterials exhibit particular properties that can overcome the drawbacks of conventional therapies such as lack of specificity, high drug concentrations, and adverse drug reactions. Among nanocarriers, mesoporous silica nanoparticles (MSNs) have gained increasing attention due to their well-defined pore size and structure, high surface area, good biocompatibility and biodegradability, ease of surface modification, and stable aqueous dispersions. This review highlights the current progress with the use of MSNs for the delivery of chemotherapeutic agents for the diagnosis and treatment of cancer. Various stimuli-responsive gatekeepers, which endow the MSNs with on-demand drug delivery, surface modification strategies for targeting purposes, and multifunctional MSNs utilized in drug delivery systems (DDSs) are also addressed. Also, the capability of MSNs as flexible imaging platforms is considered. In addition, physicochemical attributes of MSNs and their effects on cancer therapy with a particular focus on recent studies is emphasized. Moreover, major challenges to the use of MSNs for cancer therapy, biosafety and cytotoxicity aspects of MSNs are discussed.


Subject(s)
Nanoparticles , Neoplasms , Drug Carriers/chemistry , Drug Delivery Systems/methods , Humans , Nanoparticles/chemistry , Neoplasms/diagnosis , Neoplasms/drug therapy , Porosity , Silicon Dioxide/chemistry
9.
Pharmaceutics ; 14(5)2022 Apr 20.
Article in English | MEDLINE | ID: mdl-35631481

ABSTRACT

It has been hypothesized that simvastatin could be used to treat pulmonary arterial hypertension (PAH). This study is intended to formulate a simvastatin nanoparticle dry powder inhalation (DPI) formulation. Simvastatin nanoparticles were prepared via an emulsification and homogenization-extrusion method, followed by spray drying of the colloidal suspension of simvastatin nanoparticles containing mannitol to get it into a respirable size. Particle size distribution, morphology, and crystallinity of the fabricated nanoparticles of the obtained microparticles for DPI formulation were assessed by dynamic light scattering (DLS), scanning electron microscopy (SEM), and X-ray diffraction pattern (XRPD), respectively. Aerosolization performance of the DPI formulation was assessed by the Next Generation Impactor (NGI) equipped with an Aerolizer®. Simvastatin nanoparticles were around 100 nm with a very narrow size distribution (PDI = 0.105). The X-ray diffraction pattern revealed that the crystallinity of simvastatin was decreased by the spray drying procedure. Microscopic images displayed that gathered nanoparticles were in the suitable inhalable range and had the appropriate shape and surface properties for pulmonary delivery. Aerosolization assessment by the NGI indicated a suitable inhalation performance (fine particle fraction of 20%). In conclusion, the results confirmed that the spray drying technique for simvastatin can be optimized to obtain simvastatin aggregated nanoparticles without any coarse carrier to be used in DPI formulation for better deposition of the drug in the lungs for local treatment of PAH.

10.
Pharm Dev Technol ; 27(5): 525-544, 2022 Jun.
Article in English | MEDLINE | ID: mdl-35635506

ABSTRACT

The bioavailability of drugs is dependent on several factors such as solubility and the administration route. A drug with poor aqueous solubility, therefore, poses challenges with regards to its pharmaceutical advance and ultimately its biological usage. Lipid nanoparticles have been used in pharmaceutical science due to their importance in green chemistry. Their biochemical properties as 'green' materials and biochemical processes as 'green' processes mean they can be environmentally sustainable. Generally, lipid nanoparticles can be employed as carriers for both lipophilic and hydrophilic drugs. The proposed administration route for nanoparticles can present advantages and disadvantages which should be considered by a formulator. Solid lipid nanoparticles (SLNs) and nanostructured lipid carriers (NLCs) are attractive delivery systems because of their ease of manufacture, biocompatibility, biodegradability, and scale-up capacity of formulation constituents. The easy and simple scalability of novel SLNs and nano lipid carriers, along with their various processing procedures, recent developments, limitation and toxicity, formulation optimization and approaches for the manufacture of lipid nanoparticles, lyophilization and drug release are comprehensively discussed in this review. This review also summarizes the research data related to the various preparation methods and excipients used for SLNs and NLCs in recent years.


Subject(s)
Nanostructures , Drug Carriers/chemistry , Drug Delivery Systems/methods , Lipids/chemistry , Liposomes , Nanoparticles/chemistry , Nanostructures/chemistry , Particle Size
11.
AAPS PharmSciTech ; 23(5): 149, 2022 May 20.
Article in English | MEDLINE | ID: mdl-35595933

ABSTRACT

The goal of this experimentation was to increase the cutaneous absorption of venlafaxine HCl (VFX) encapsulated in a niosome (venlasosme) produced by an ultrasonic approach. The impact of the cholesterol:surfactant (Chol:Surf) proportion was examined to modify the venlasosme properties. Photon correlation spectroscopy, powder X-ray diffraction (PXRD), SEM, DSC, and ATR-FTIR spectroscopy were utilized to investigate the solid-state and morphology of VFX in the venlasosme. The studies revealed that increasing the level of Chol in the venlasosme increased the size of the particles. Alterations in the Chol to surfactant ratios (when Chol decreased from 2.5 to 0%) caused the zeta potential enhancement from 7.37 ± 0.67 to 15.53 ± 1.47 mV. The venlasosme with the highest cholesterol concentration (2.5%) had the highest encapsulation efficiency (approximately 63%). PXRD results revealed that VFX in venlasosme was in the amorphous form. The levels of VFX in the cutaneous layers and the receiver compartment were higher for the venlasosme gel than for VFX simple gel in the cutaneous permeability study and showed no cutaneous irritancy in rats. Furthermore, the venlasosme gel demonstrated significant antinociceptive and anti-inflammatory responses when compared to the control groups (VFX simple gel and diclofenac gel). The topical administration of the venlasosme gel also considerably increased the tail-flick and hot-plate response time when compared to the VFX simple gel, control groups, and diclofenac gel (p < 0.05). These findings suggest that niosomes can improve VFX efficacy as an antinociceptive and anti-inflammatory substance by improving the medicaments delivery to the specified site.


Subject(s)
Diclofenac , Liposomes , Analgesics , Animals , Anti-Inflammatory Agents , Cholesterol , Pain/drug therapy , Rats , Surface-Active Agents , Venlafaxine Hydrochloride
12.
AAPS PharmSciTech ; 23(3): 81, 2022 Mar 09.
Article in English | MEDLINE | ID: mdl-35266075

ABSTRACT

The present study aimed to formulate atorvastatin niosome (Atrosome) through an ultrasonic technique and to determine its contribution to the extent of wound healing in an animal model. The optimized Atrosome formulation (Atrosome-2) was stable at 4 °C for 3 months. Differential scanning calorimetry (DSC), ATR-Fourier transform infrared spectroscopy (ATR-FTIR), and powder X-ray diffraction (PXRD) analysis revealed that atorvastatin (ATR) was well encapsulated within the niosomes either in a stabilized amorphous form or a molecularly dispersed state. Scanning electron microscopy (SEM), transmission electron microscopy (TEM), and atomic force microscope (AFM) confirmed the spherical nature of the Atrosomes. The optimized formulation showed polydispersity index, particle size, drug encapsulation efficiency (EE%), and zeta potential of 0.457 ± 0.05, 196.33 ± 6.45 nm, 86.15 ± 0.58 %, and - 20.73 ± 0.98 mV, respectively. ATR release from the Atrosome gel followed the first-order kinetic model and showed no cytotoxicity in the in vitro cytotoxicity test. Cell viability (human foreskin fibroblast cell line) was nearly 99%. An excision wound model was also applied in male Wistar rats to examine the in vivo efficacy of the optimized formulation, followed by investigating malondialdehyde (MDA, an end-product of lipid peroxidation), superoxide dismutase (SOD, an endogenous antioxidant), hydroxyproline levels, and glutathione peroxidase (GPx) in skin tissue samples. MDA significantly decreased in the Atrosome gel group after 21 days, while GPx, SOD, and hydroxyproline levels demonstrated an increase. According to histological results, rats receiving Atrosomes were treated effectively faster when compared to the other formulation used.


Subject(s)
Liposomes , Nanoparticles , Animals , Atorvastatin/pharmacology , Calorimetry, Differential Scanning , Male , Nanoparticles/chemistry , Particle Size , Rats , Rats, Wistar , Wound Healing
13.
J Drug Target ; 30(1): 108-117, 2022 01.
Article in English | MEDLINE | ID: mdl-34116599

ABSTRACT

The purpose of this research was to enhance the transdermal delivery of diclofenac sodium niosomal formulations. To characterise the obtained niosomes, SEM, XRPD, DSC and ATR-FTIR were employed. The size of the niosomes increased from 158.00 ± 6.17 to 400.87 ± 4.99 nm when cholesterol was incorporated into the formulations. It was observed that the zeta potential of niofenac varies from -25.40 ± 1.352 to -43.13 ± 1.171 mV when the cholesterol percentage decreased from 2% to 0.2%. The higher entrapment efficiency percentage (63.70 ± 0.18%) was obtained for the formulations with larger particle sizes and higher cholesterol content. The optimised niofenac formulation showed a controlled release fashion where 61.71 ± 0.59% of the drug released within 24 h. The results showed that the value of permeated diclofenac sodium through the skin layers was higher for the niofenac gel formulation (242.3 ± 31.11 µg/cm2) compared to simple gel formulation (127.40 ± 27.80 µg/cm2). Besides, niofenac formulation outperformed the anti-inflammatory activities in the formalin test compared to the control and diclofenac simple gel group. The licking time was significantly lower in both early (40.2 ± 7.3 s) and late stages (432.4 ± 31.7 s) for niofenac compared to conventional formulation (early stage 130.4 ± 8.73 s and late stage 660.6 ± 123.73 s). This study indicates that niosomal formulations can improve drug therapeutic effects by increasing drug delivery to specific sites.


Subject(s)
Diclofenac , Liposomes , Administration, Cutaneous , Drug Delivery Systems/methods , Gels , Particle Size
14.
Drug Discov Today ; 27(2): 471-489, 2022 02.
Article in English | MEDLINE | ID: mdl-34781032

ABSTRACT

The uncontrolled release of drugs in conventional drug delivery systems has led to the introduction of new nanotechnology-based drug delivery systems and the use of targeted nanocarriers for cancer treatment. These targeted nanocarriers, which consist of intelligent nanoparticles modified with targeting ligands, can deliver drugs to specified locations at the right time and reduce drug doses to prevent side effects. Folate is a suitable targeting ligand for folate receptors overexpressed on cancer cells and has shown promising results in the diagnosis and treatment of cancer. In this review, we highlight the latest developments on the use of folate-conjugated nanoparticles in cancer diagnosis and treatment. Moreover, the toxicity, biocompatibility and efficacy of these nanocarriers are discussed.


Subject(s)
Nanoparticles , Neoplasms , Drug Carriers/therapeutic use , Drug Delivery Systems/methods , Folic Acid/therapeutic use , Humans , Ligands , Neoplasms/drug therapy
15.
Pharm Dev Technol ; 27(1): 63-71, 2022 Jan.
Article in English | MEDLINE | ID: mdl-34939892

ABSTRACT

Pistacia atlantica has an anti-cancer effect due to its essential oil which is the major constituent of P. atlantica. Unfortunately, this essential oil evaporates easily and makes it less effective. The current research, therefore, aimed to improve the anti-cancer effect of P. atlantica essential oil (PAEO) in solid lipid nanoparticles (SLN). The chemical components of PAEO were assessed by gas chromatography. PAEO-SLNs were prepared by the probe-ultrasonication method, and their particle size, polydispersity index and zeta potential were determined. Encapsulation Efficiency (EE%) and Loading Capacity (LC%) of formulations was also calculated. Transmission electron microscopy was employed to determine the morphology of optimal formulation (PAEO-SLN4). Furthermore, the anticancer effects of PAEO-SLN4 against MDA-MB-231 cells were evaluated by cellular assays. The results showed that the type of surfactant and loading of the essential oil had a significant effect on size distribution, zeta potential and the polydispersity index. The encapsulation efficiency (EE%) and loading capacity for PAEO-SLN4 were 97.3% and 9.6%, respectively. The cellular assay demonstrates that PAEO-SLN4 could lead MDA-MB-231 cells to apoptosis. The findings also revealed that PAEO-SLN4 can stimulate apoptosis in MDA-MB-231 cells more than the placebo and free PAEO thereby indicating PAEO-SLN4 to be beneficial in breast cancer treatment.


Subject(s)
Breast Neoplasms , Nanoparticles , Oils, Volatile , Pistacia , Apoptosis , Breast Neoplasms/drug therapy , Cell Line , Female , Humans , Liposomes , Nanoparticles/chemistry , Oils, Volatile/pharmacology , Particle Size
16.
Bioimpacts ; 12(6): 561-566, 2022.
Article in English | MEDLINE | ID: mdl-36644547

ABSTRACT

Introduction: This study was proposed to assess the potential role of efflux transporters in reversing fluconazole resistance in Candida glabrata isolates treated with fluconazole loaded nanostructured lipid carriers (FLZ-NLCs). Methods: The ultrasound technique was used to synthesize the FLZ-NLCs. Four fluconazole-resistant, as well as one susceptible standard C. glabrata isolates, were applied and exposed to FLZ/ FLZ-NLCs for 20 h at 37°C. Real-time PCRs were done to estimate the likely changes in ATP-binding cassette transporter genes. Results: Similar to the FLZ-exposed-susceptible standard strain which showed no alteration, the genes were not up-regulated significantly under the FLZ-NLCs treated condition. While they were over-expressed when the yeasts were treated with fluconazole. Conclusion: It is highly suggested that due to the nature of the NLCs which shields the whole conformation of the drug, FLZ is not recognized by the efflux transporter subunits and consequently the translocation would not happen.

17.
AAPS PharmSciTech ; 23(1): 42, 2021 Dec 28.
Article in English | MEDLINE | ID: mdl-34964076

ABSTRACT

Solubility determination of poorly water-soluble drugs is pivotal for formulation scientists when they want to develop a liquid formulation. Performing such a test with different ratios of cosolvents with water is time-consuming and costly. The scarcity of solubility data for poorly water-soluble drugs increases the importance of developing correlation and prediction equations for these mixtures. Therefore, the aim of the current research is to determine the solubility of acetylsalicylic acid in binary mixtures of ethanol+water at 25 and 37°C. Acetylsalicylic acid is non-stable in aqueous solutions and readily hydrolyze to salicylic acid. So, the solubility of acetylsalicylic acid is measured in ethanolic mixtures by HPLC to follow the concentration of produced salicylic acid as well. Moreover, the solubility of acetylsalicylic acid is modeled using different cosolvency equations. The measured solubility data were also predicted using PC-SAFT EOS model. DSC results ruled out any changes in the polymorphic form of acetylsalicylic acid after the solubility test, whereas XRPD results showed some changes in crystallinity of the precipitated acetylsalicylic acid after the solubility test. Fitting the solubility data to the different cosolvency models showed that the mean relative deviation percentage for the Jouyban-Acree model was less than 10.0% showing that this equation is able to obtain accurate solubility data for acetylsalicylic acid in mixtures of ethanol and water. Also, the predicted data with an average mean relative deviation percentage (MRD%) of less than 29.65% show the capability of the PC-SAFT model for predicting solubility data. A brief comparison of the solubilities of structurally related solutes to acetylsalicylic acid was also provided.


Subject(s)
Ethanol , Water , Aspirin , Solubility , Solvents
18.
Adv Drug Deliv Rev ; 177: 113949, 2021 10.
Article in English | MEDLINE | ID: mdl-34461199

ABSTRACT

UV-vis spectrometry is widely used in the pharmaceutical sciences for compound quantification, alone or in conjunction with separation techniques, due to most drug entities possessing a chromophore absorbing light in the range 190-800 nm. UV dissolution imaging, the scope of this review, generates spatially and temporally resolved absorbance maps by exploiting the UV absorbance of the analyte. This review aims to give an introduction to UV dissolution imaging and its use in the determination of intrinsic dissolution rates and drug release from whole dosage forms. Applications of UV imaging to non-oral formulations have started to emerge and are reviewed together with the possibility of utilizing UV imaging for physical chemical characterisation of drug substances. The benefits of imaging drug diffusion and transport processes are also discussed.


Subject(s)
Drug Liberation , Ultraviolet Rays , Dosage Forms , Drug Delivery Systems , Pharmaceutical Preparations/administration & dosage , Pharmaceutical Preparations/chemistry
19.
Sci Rep ; 11(1): 15603, 2021 08 02.
Article in English | MEDLINE | ID: mdl-34341399

ABSTRACT

The therapeutic effectiveness of a chitosan encapsulated bacteriophage cocktail as a smart biocontrol agent was evaluated in this study to be used as a preventative and treatment option for gastrointestinal infections. To evaluate the effect of the bacteriophage formulation on the treatment of gastrointestinal infection, rats were infected with Salmonella enterica, Shigella flexneri, and Escherichia coli. The rats were weighed and their stools cultured. The results showed that the group which had the chitosan encapsulated bacteriophage cocktail did not lose weight after 3 days and had significantly lower group weight changes. Weight loss was significant in the rats that had cefixime administered instead. Positive cultured stools were reduced after 4 days compared to 2 days in the treated group with the chitosan encapsulated bacteriophage cocktail. The chitosan encapsulated bacteriophage cocktail can therefore be effective in the treatment of gastrointestinal infections.


Subject(s)
Bacteriophages , Chitosan , Shigella flexneri , Food Microbiology
20.
Biomedicines ; 9(8)2021 Aug 07.
Article in English | MEDLINE | ID: mdl-34440179

ABSTRACT

The purpose of this study was to prepare poly (D-L) lactide-co-glycolide (PLGA) and poly ε-caprolactone (PCL) nanofibers containing metronidazole and amoxicillin using an electrospinning process as intrapocket sustained-release drug delivery systems for the treatment of periodontal diseases. Scanning electron microscopy showed that the drug containing PLGA and PCL nanofibers produced from the electrospinning process was uniform and bead-free in morphology. The obtained nanofibers had a strong structure and resisted external tension according to the tensiometry results. The cytotoxicity results indicated acceptable cell viability (>80%). Quantification by high-performance liquid chromatography showed almost complete in vitro drug release between 7 and 9 days, whereas 14 days were required for complete drug release in vivo. No significant signs of irritation or inflammatory reaction were detected after three weeks of subcutaneous implantation of nanofibers in the animal models, thus indicating suitable compatibility. The results therefore suggest that the designed nanofibers can be used as potential commercial formulations in the treatment of periodontitis as controlled-release intrapocket drug delivery systems that can increase patient compliance. This is due to their ability to reduce the frequency of administration from three times daily in a systemic manner to once weekly as local delivery.

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