Letrozole (LZ) is an aromatase inhibitor, which inhibits the formation of estrogens from androgens. Nanoemulsion is a liquid emulsion formulation utilized to increase solubility, bioavailability, and drug delivery to cancer cells. This study aims to improve LZ oral delivery through formulating solid nanoemulsion (SNE). Peppermint oil, tween 80, and transcutol P were used as an oil, surfactant, and co-surfactant, respectively. The optimized nanoemulsion (NE-3) was then incorporated into solid polyethylene glycol (PEG) to formulate (SNE). The optimized (NE-3), SNE-2, and the available marketed tablet have been compared. The optimized (NE-3) was selected according to specific parameters of optimum small nano-size 80 nm, PDI of 0.181, the zeta potential of-98.2, high transmittance (99.78%), optimum pH (5.6), a high percent of LZ content (99.03 ± 1.90), the relatively low viscosity of 60.2 mPa.s, and a rapid release of LZ within 30 min. NE-3 was selected to be formulated as SNE. LZ's best release rate was 80% in 5 min with a content homogeneity of 99.85 ± 0.04 for SNE-2. Zero-order kinetics is determined to have the greatest R 2 values. Field emission scanning electron microscopy (FE-SEM) detected that SNE-2 was (36.75–96.64 nm) with a spherical form and no adhesion or aggregation. FT-IR showed no significant variations in position and shape of the absorption peaks between the pure drug and optimal formulation diagrams. This novel nanoemulsion technology aids in improving the solubility of poorly water-soluble drugs, particularly the SNE delivery method, which has a higher in-vitro release rate and expiration date of LZ than others.
Objective: The object of this study was to improve flurbiprofen permeability transdermally using castor oil as penetration enhancer. Methods:Castor oil with different concentrations (1%, 2%, 3%, 4%, and 5%) was used in this study as a natural enhancer to improve flurbiprofen permeation transdermally as a gel. The formulated gel of the drug was evaluated for several physicochemical characteristics. The in vitro release and permeability studies for the drug were performed using Franz cell diffusion apparatus across the synthetic membrane. Korsmeyer Pappas kinetic model was used to study the release mechanism of flurbiprofen from the gel. Results:The results demonstrated that castor oil was safe with no skin irritation and the formulas were stable over time. Castor oil was significantly effective in increasing the percent of flurbiprofen permeability from 46%±2.9 for the gel without enhancer to 95%±2 for the gel with 5% castor oil and increasing its penetration is directly related to the oil concentration. Two mechanisms for the drug release from the gel were involved, which are non-Fickian (anomalous) and super case II transport. Conclusion:Flurbiprofen gel was prepared and evaluated successfully for an in vitro parameters with a good permeation across a synthetic membrane. The results demonstrated that castor oil had an effective enhancement for permeation of flurbiprofen.
Objective: The objective of our current work is to formulate, optimize and evaluate new combination rectal suppositories as a treatment for rheumatoid arthritis that contains both lornoxicam and aloin. Both are strong anti-inflammatory agents, and a combination of both may have synergistic effect as an anti-inflammatory treatment.Methods: Rectal suppositories containing 8 mg lornoxicam and 200 mg aloin were formulated by heat fusion method. Different combinations of different molecular weights of polyethylene glycol (PEG) were used for the formulated suppositories. The formulated suppositories were evaluated for their visual appearance, weight variation, hardness, friability, disintegration time, melting temperature, and drug content uniformity.Results: All the formulations prepared were within the required limits for USP. When the release study was performed, both drugs were released from all the formulations prepared. However, formulation F7 which is composed of PEG 400 30.88% (w/w): PEG 4000 46.32% (w/w) was superior to other formulations in which more than 80% of both drugs loaded were released after 35 min. The presence of both drugs in the same suppository did not affect their release.Conclusion: A new combination suppositories have been obtained where the two combined drugs were released fast without interference with each other release. The proposed new combination has the potential to be used as a strong analgesic and anti-inflammatory treatment compared to using lornoxicam or aloin alone.
Fast-dissolving films are one of the interested delivery systems for oral solid dosage forms to overcome swallowing difficulty for geriatric and pediatric patients. Zafirlukast (ZLK) is one of the most commonly used oral medication for treatment of asthmatic patients particularly mild to moderate cases. Oral fast dissolving films of ZLK were prepared using two different filming forming polymers, hydroxypropyl methylcellulose (HPMC) and sodium carboxymethyl cellulose (SCMC). Different concentrations of the 2 polymers were used to prepare 10 formulas. Other excipients were also added at various ratios to produce 10 different formulations. These were maltodextrin, crosspivodone, polyvinylpyrrolidone (PVP), and banana powder. In vitro characterization of the formulations showed that HPMC-based formulations had significantly shorter disintegrating times (p < 0.05) and improved dissolution rates. Addition of crosspovidone, PVP, and maltodextrin as disintegrants to the film forming polymers did not significantly enhance the disintegration of the films. However, banana powder significantly elongated the film disintegration. Compatibility studies using FTIR did not show an interaction between ZLK and excipients in all formulations.
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