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1.
PLoS One ; 19(5): e0303060, 2024.
Article in English | MEDLINE | ID: mdl-38723008

ABSTRACT

In the current study we investigated the impact of combination of rutin and vitamin A on glycated products, the glyoxalase system, oxidative markers, and inflammation in animals fed a high-fat high-fructose (HFFD) diet. Thirty rats were randomly divided into six groups (n = 5). The treatments, metformin (120 mg/kg), rutin (100 mg/kg), vitamin A (43 IU/kg), and a combination of rutin (100 mg/kg) and vitamin A (43 IU/kg) were given to relevant groups of rats along with high-fructose high-fat diet for 42 days. HbA1c, D-lactate, Glyoxylase-1, Hexokinase 2, malondialdehyde (MDA), glutathione peroxidase (GPx), catalase (CAT), nuclear transcription factor-B (NF-κB), interleukin-6 (IL-6), interleukin-8 (IL-8) and histological examinations were performed after 42 days. The docking simulations were conducted using Auto Dock package. The combined effects of rutin and vitamin A in treated rats significantly (p < 0.001) reduced HbA1c, hexokinase 2, and D-lactate levels while preventing cellular damage. The combination dramatically (p < 0.001) decreased MDA, CAT, and GPx in treated rats and decreased the expression of inflammatory cytokines such as IL-6 andIL-8, as well as the transcription factor NF-κB. The molecular docking investigations revealed that rutin had a strong affinity for several important biomolecules, including as NF-κB, Catalase, MDA, IL-6, hexokinase 2, and GPx. The results propose beneficial impact of rutin and vitamin A as a convincing treatment strategy to treat AGE-related disorders, such as diabetes, autism, alzheimer's, atherosclerosis.


Subject(s)
Diet, High-Fat , Fructose , Hyperglycemia , Inflammation , Oxidative Stress , Rutin , Vitamin A , Animals , Rutin/pharmacology , Oxidative Stress/drug effects , Fructose/adverse effects , Rats , Diet, High-Fat/adverse effects , Vitamin A/pharmacology , Vitamin A/metabolism , Inflammation/metabolism , Inflammation/drug therapy , Inflammation/pathology , Male , Hyperglycemia/drug therapy , Hyperglycemia/metabolism , Hyperglycemia/chemically induced , Molecular Docking Simulation , Rats, Wistar , Disease Models, Animal , Glycosylation/drug effects , Metformin/pharmacology , Glycated Hemoglobin/metabolism , NF-kappa B/metabolism , Hexokinase/metabolism , Catalase/metabolism
2.
Pak J Pharm Sci ; 37(1(Special)): 215-222, 2024 Jan.
Article in English | MEDLINE | ID: mdl-38747272

ABSTRACT

This study was aimed to assess the type and severity of COVID vaccine-induced menstrual disorders and also to investigate the risk factors for menstrual changes following COVID-19 vaccination in Pakistani females. A cross-sectional survey-based study was conducted in females between 12 -70 years of age from February to July 2022. The survey was conducted via in-person interviews as well as via social media. The data was analyzed using standard descriptive statistical parameters, the sociodemographic and clinical features were evaluated and reported as frequencies (percentages). The study comprised a total of 1023 female subjects. Approximately 36.9% of women reported menstrual abnormalities following immunization, with 30.5% experiencing them following their second dose. However, in majority of these women (21%) the symptoms were resolved after 3 months of irregularity. Vaccine type significantly influenced the incidence of menstrual disorders (p <0.001) which were linked to Pfizer-Biontech, Sinopahrm, Sinovac, Moderna at rates of 14.9%, 9.5%, 4.7% and 2.7%, respectively. Both AstraZeneca and Moderna were implicated in postmenopausal bleeding (1.6% and 0.8%, respectively). The study showed that females receiving COVID-19 vaccines experienced menstrual irregularities such as short duration of periods, decreased volume of bleeding, and frequent menstrual cycles. However, the symptoms were temporary and self-limiting.


Subject(s)
COVID-19 Vaccines , COVID-19 , Menstruation Disturbances , Humans , Female , Cross-Sectional Studies , Pakistan/epidemiology , Adult , COVID-19 Vaccines/adverse effects , COVID-19 Vaccines/administration & dosage , Adolescent , Middle Aged , Young Adult , COVID-19/prevention & control , COVID-19/epidemiology , Menstruation Disturbances/epidemiology , Aged , Child , Risk Factors , SARS-CoV-2/immunology , Vaccination/adverse effects
3.
Saudi Pharm J ; 31(12): 101860, 2023 Dec.
Article in English | MEDLINE | ID: mdl-38192284

ABSTRACT

Croton bonplandianus, a natural source traditionally used for treating various illnesses, including rheumatoid arthritis, was evaluated in this study. The effects of ethanolic extracts (CBEE) and aqueous fractions (CBAF) of C. bonplandianus leaves on arthritis-induced inflammation were studied using an albino rat model of inflammation induced by Freund's complete adjuvant. Eight test groups (n = 5 per group) and one vehicle control were used to evaluate the antiarthritic effects of different doses of CBEE and CBAF (125 mg.kg-1, 250 mg.kg-1, and 500 mg.kg-1) on days 5, 10, 15, and 20 compared to arthritic and vehicle controls. Arthritis severity was assessed using macroscopic arthritis grading, histological analysis, body weights, and paw thickness. CBEE and CBAF were found to reduce the prevalence of arthritis, increase body weight, and decrease paw inflammation compared to the vehicle control group by the 23rd day. In addition, they showed no effect on biochemical parameters, but a significant difference (p < 0.05) in hematological parameters compared to the arthritic control group. The study identified Hentriacontane compound as a potential contributor to the anti-inflammatory effect of C. bonplandianus, as it showed the lowest dock score for IL-1ß and IL-6. Palmitoylethanol amide was identified as a potential contributor to the anti-inflammatory effect of TNF-α. Gene expression of IL-6, IL-1ß, and TNF-α was down-regulated significantly (p < 0.05) in a dose-dependent manner in all treatment groups compared to the arthritic control group. In conclusion, this study validated the anti-arthritic and anti-inflammatory properties of CBEE and CBAF in a time and dose-dependent manner.

4.
Pak J Pharm Sci ; 35(4): 1007-1014, 2022 Jul.
Article in English | MEDLINE | ID: mdl-36008896

ABSTRACT

Orodispersible film (ODF) is a better alternate to oral disintegrating tablets owing to its ease in application and subsequent patient compliance. This study investigates an improvement in physico-mechanical properties and palatability of Diltiazem Hydrochloride (DTZ) by formulating ODF employing solvent casting method. DTZ, used in the treatment of angina and hypertension, undergoes extensive presystemic metabolism and gives an incomplete bioavailability of 35-40%. DTZ also manifests a very bitter taste and after taste. DTZ was formulated into films using different polymer concentrations of Hydroxypropyl methylcellulose ethocel5 and Carboxymethyl cellulose and plasticizer levels of Propylene glycol and Glycerin to screen appropriate polymer-plasticizer combination. Optimized film disintegrated in 10.0±1.53 sec and appeared to be clear and smooth and almost 100% of the drug release was achieved within 4min from the ODF. Film revealed a good mechanical strength with folding endurance of >260, tensile strength of 1.36±0.11 N/mm2 and % elongation of 15.47±0.47%. FTIR and DSC showed compatibility between the drug and polymer. Film demonstrated a slightly sweet taste and after taste as well as an acceptability by the human volunteers. In conclusion DTZ was successfully formulated into film with improved physical properties and taste and could be beneficial to patients with cardiovascular disorders.


Subject(s)
Diltiazem , Taste , Administration, Oral , Chemistry, Pharmaceutical/methods , Humans , Plasticizers , Polymers , Solubility , Tablets
5.
Pharmaceuticals (Basel) ; 15(7)2022 Jul 14.
Article in English | MEDLINE | ID: mdl-35890167

ABSTRACT

Plant mucilages are commonly employed as excipients in pharmaceutical manufacturing. Ocimum basilicum (Lamiaceae family), a source of hydrophilic mucilage referred herein as Ocicum, was evaluated for the solubility enhancer of a model drug, aceclofenac, in solid dispersions prepared using different methods. Polymer was extracted from O. basilicum and solid dispersions of aceclofenac were fabricated with Ocicum or Poloxamer 407 using polymer-to-drug ratios of 1:1, 1:2 and 1:3 utilizing solvent evaporation, lyophilization and melt methods. Ocicum was evaluated for its safety via acute toxicity study including different biochemical and hematological parameters including liver and kidney profiles. Moreover, different characterization studies including melting-point, Fourier transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and differential thermal analysis (TGA) were used for evaluation of polymer and solid dispersions. Furthermore, solubility and dissolution studies were performed to confirm solubility enhancement. Ocicum was found to be safer, and different characterization studies confirmed the purity of the compounds. In addition, Ocicum exhibited up to 6.27-fold enhanced solubility as compared to pure aceclofenac; similarly, 4.51-fold increased solubility by the synthetic polymer in their respective solid dispersions was shown. Furthermore, Ocicum-based solid dispersions showed substantial improvement in dissolution of aceclofenac. Therefore, it can be concluded from the above-mentioned results that Ocicum might be used as an economical natural oral delivery carrier alternative to the synthetic polymers.

6.
Medicina (Kaunas) ; 55(1)2019 Jan 11.
Article in English | MEDLINE | ID: mdl-30642012

ABSTRACT

Background and objectives: Turmeric has assisted in the control of inflammation and pain for decades and has been used in combination with other nutraceuticals to treat acute and chronic osteoarthritis pain. Recently, the effect of turmeric, turmeric extract, or curcuminoids on musculoskeletal pain, either by themselves or in conjunction with other substances, has been reported. The aim of this study was to develop and characterize turmeric nanoparticles (T-NPs) for various parameters, both in vitro and in vivo. Materials and Methods: The T-NPs were successfully synthesized and characterized using particle size analysis, solubility improvement, SEM, EDX, X-ray diffraction, and in vivo antigout activity in mice model. Results: The T-NPs were of about 46 nm in size with a positive zeta potential +29.55 ± 3.44 and low polydispersity index (PDI) (0.264). Furthermore, the diseased mice, with induced gout via monosodium urate crystals, were treated with 5, 10, and 20 ppm T-NPs, administered orally, and the anti-gout potential was observed through measurement of joint diameter and changes in biochemical parameters, including lipid profile, renal function test, and liver function tests which significantly reduced the levels of these biochemical parameters. Conclusions: Uric acid levels were significantly reduced after the treatment with T-NPs. indicating that T-NPs show superior potential against gout management. Thus, T-NPs can be developed as an efficient antigout agent with minimum toxicities.


Subject(s)
Curcuma , Gout Suppressants/administration & dosage , Gout/drug therapy , Nanoparticles/administration & dosage , Phytotherapy , Plant Extracts/administration & dosage , Animals , Antioxidants/chemical synthesis , Antioxidants/pharmacology , Cholesterol, HDL/blood , Cholesterol, LDL/blood , Curcuma/chemistry , Disease Models, Animal , Drug Delivery Systems , Dynamic Light Scattering , Gout/blood , Gout/chemically induced , Gout/pathology , Gout Suppressants/chemistry , Kidney Function Tests , Liver Function Tests , Mice , Nanoparticles/chemistry , Plant Extracts/chemistry , Spectrum Analysis , Triglycerides/blood , Uric Acid/blood , Uric Acid/chemical synthesis , Uric Acid/pharmacology , X-Ray Diffraction
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