Aceclofenac/Citronellol Oil Nanoemulsion Repurposing Study: Formulation, In Vitro Characterization, and In Silico Evaluation of Their Antiproliferative and Pro-Apoptotic Activity against Melanoma Cell Line.

Aceclofenac (ACF) is a widely used non-steroidal anti-inflammatory drug (NSAID) known for its effectiveness in treating pain and inflammation. Recent studies have demonstrated that ACF possesses antiproliferative properties, inhibiting the growth of cancer cells in various cancer cell lines. Citronellol, a monoterpenoid alcohol found in essential oils, exhibits antioxidant properties and activities such as inhibiting cell growth and acetylcholinesterase inhibition. In this study, the objective was to formulate and evaluate an aceclofenac/citronellol oil nanoemulsion for its antiproliferative effects on melanoma. The optimal concentrations of citronellol oil, Tween 80, and Transcutol HP were determined using a pseudoternary phase diagram. The formulated nanoemulsions were characterized for droplet size, zeta potential, thermophysical stability, and in vitro release. The selected formula (F1) consisted of citronellol oil (1 gm%), Tween 80 (4 gm%), and Transcutol HP (1 gm%). F1 exhibited a spherical appearance with high drug content, small droplet size, and acceptable negative zeta potential. The amorphous state of the drug in the nanoemulsion was confirmed by Differential Scanning Calorimetry, while FTIR analysis indicated its homogenous solubility. The nanoemulsion showed significant antiproliferative activity, with a lower IC50 value compared to aceclofenac or citronellol alone. Flow cytometric analysis revealed cell cycle arrest and increased apoptosis induced by the nanoemulsion. In silico studies provided insights into the molecular mechanism underlying the observed antitumor activity. In conclusion, the developed aceclofenac/citronellol oil nanoemulsion exhibited potent cytotoxicity and pro-apoptotic effects, suggesting its potential as a repurposed antiproliferative agent for melanoma treatment. In a future plan, further animal model research for validation is suggested.

Ketoprofen mesoporous silica nanoparticles SBA-15 hard gelatin capsules: preparation and in vitro/in vivo characterization.

SBA-15 is used to enhance the bioavailability of poorly soluble ketoprofen (KP) through stabilization of its amorphous state. Additionally, the current work provides a complete in vitro and in vivo study on preformulated KP-SBA-15 sample and formulated KP-SBA-15 in hard gelatin capsule. Loading of KP was done by a novel method called immersion-rotavapor method. KP was quantified by extraction and thermal gravimetric analysis (TGA). Characterization of the loaded SBA-15 sample was done by high resolution transmission electron microscopy (HRTEM), small angle X-ray diffraction (SAXRD), nitrogen adsorption/desorption isotherms, differential scanning calorimetry (DSC), Fourier transform infrared (FT-IR) spectroscopy and dissolution profiles. The loaded sample was formulated in hard gelatin capsule. The anti-inflammatory and analgesic studies were carried out on 24 adult male albino rats. TGA and extraction results showed 54.4 wt% of drug incorporated. Characterization of KP-SBA-15 sample confirmed the successful encapsulation of KP into the carrier pores in a molecular amorphous state. Additionally, loading of KP did not affect the mesoporous internal structure. During the first 5 min, the dissolution study showed very high release rates; nearly 50% of KP was released. These results were reflected on the in vivo study resulting in 82% inhibition in edema after 1 h and maximum analgesia after 30 min from the administration of the formulated sample. SBA-15 mesoporous silica nanoparticle proved to be a very promising drug delivery carrier that can be used as a facile way to enhance the bioavailability of poorly soluble drugs.

Risk factors for falls in a longitudinal cohort study of Saudi postmenopausal women: the Center of Excellence for Osteoporosis Research Study.

OBJECTIVE: This study aims to identify possible risk factors for falls among Saudi postmenopausal women in a population-based study. METHODS: Seven hundred seven postmenopausal women aged 50 years or older were followed in a prospective cohort study. Participant demographic characteristics, medical history, lifestyle factors, past-year history of falls, and physical activity (PA) scores were assessed. We recorded single and multiple falls, anthropometric parameters, five special physical performance tests, hormone levels, and bone mineral density measurements. Data on knee osteoarthritis (OA), lumbar spondylosis, and osteopenia were collected. Knee and lower back pain were assessed by interview, and cognition was assessed with Mini-Mental State Examination. RESULTS: During the mean (SD) follow-up of 5.2 (1.3) years, 164 women (23.2%) reported at least one fall, of whom 73 women (10.3%) reported multiple falls. Six independent predictors of all falls were identified: PA score of 12.61 or lower (lowest quartile; odds ratio [OR], 4.10; 95% CI, 1.82-8.90); past-year history of falls (OR, 2.44; 95% CI, 2.30-2.90); age 65 years or older (OR, 2.16; 95% CI,1.30-3.12); presence of knee OA (OR, 1.56; 95% CI,1.03-2.34); handgrip strength of 13.88 kg or lower (lowest quartile; OR, 1.33; 95% CI,1.09-1.64); and 8-ft walk test of 3.94 s or longer (highest quartile; OR, 1.18; 95% CI, 1.07-1.35). CONCLUSIONS: Poor PA score, past-year history of falls, age 65 years or older, presence of knee OA, poor handgrip strength, and prolonged time on the 8-ft walk test are risk factors for all falls among Saudi postmenopausal women.