The aim of this work was to investigate alternative safe and effective permeation enhancers for buccal peptide delivery. Basic amino acids improved insulin solubility in water while 200 and 400 μg/mL lysine significantly increased insulin solubility in HBSS. Permeability data showed a significant improvement in insulin permeation especially for 10 μg/mL of lysine (p < 0.05) and 10 μg/mL histidine (p < 0.001), 100 μg/mL of glutamic acid (p < 0.05) and 200 μg/mL of glutamic acid and aspartic acid (p < 0.001) without affecting cell integrity; in contrast to sodium deoxycholate which enhanced insulin permeability but was toxic to the cells. It was hypothesized that both amino acids and insulin were ionised at buccal cavity pH and able to form stable ion pairs which penetrated the cells as one entity; while possibly triggering amino acid nutrient transporters on cell surfaces. Evidence of these transport mechanisms was seen with reduction of insulin transport at suboptimal temperatures as well as with basal-to-apical vectoral transport, and confocal imaging of transcellular insulin transport. These results obtained for insulin are the first indication of a possible amino acid mediated transport of insulin via formation of insulin-amino acid neutral complexes by the ion pairing mechanism.
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 investigation was to formulate and evaluate effervescent granules of ibuprofen, to increase its dissolution rate to get rapid analgesic and antipyretic effects. Methods: Five formulas (F1-F5) of effervescent ibuprofen granules were formulated by the wet granulation method. Croscarmellose sodium, powder of banana and other ingredients were used in the formulation of effervescent granules. Evaluation studies were carried out for all five formulas, these include: (compatibility study, flowability study, % of drug content, effervescent time and in vitro dissolution study). Results: The results show that the formulated granules have good flow properties with suitable bulk density for the uniting dose. FTIR study shows that there is no drug interaction with other ingredients in the formula. All five formulas have effervescent time less than 3 min, F5 show the best drug release 99.1±1 and effervescent time about 80 sec. Conclusion: Ibuprofen was successfully formulated and evaluated as effervescent granules by using a combination of croscarmellose sodium and banana powder.
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.
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