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Objective: Develop and assess a transdermal emulsion loaded with nanostructured lipid carriers for vitamin D3 supplementation. Methods: Vitamin D3 loaded nanostructured lipid carriers, produced via high shear homogenization and ultrasonication, were assessed for their particle size, distribution, morphology, zeta potential, entrapment efficiency, and cytotoxicity. They were incorporated into a transdermal vehicle, and the stability and ex vivo permeation were evaluated. Results: Spherical nanoparticles were developed with a particle size of 192.5 nm, a polydispersity index of 0.13, a zeta potential of -29.0 mV, and an entrapment efficiency of 99.75%. They were stable (particle size and distribution) for 15 days when stored in a refrigerator, and for 30 days at room temperature and 32 °C. The nanoparticles decreased the drug cytotoxicity against fibroblasts, as shown by IC50 (nanoparticle: 32.48 μg mL−1; vitamin D3: 16.73 μg mL−1). The emulsion loaded with nanoparticles minimized the degradation of vitamin D3 when compared with the nanoparticle dispersion. Additionally, the emulsion provided the skin permeation of vitamin D3 following the recommended daily allowance. Conclusion: To the best of our knowledge, this is the first study to use nanostructured lipid carriers for transdermal delivery of vitamin D. The developed formulation is a promising strategy to overcome the vitamin D3 variable oral bioavailability. It also represents a comfortable route of administration; thus it could be beneficial for patients and clinicians. However, further studies are needed to allow the permeation of larger amounts of vitamin D3, and the combination of these nanoparticles with microneedles would be interesting.

Background: Transdermal delivery is an alternative route for the administration of drugs. However, it requires the development of vehicles that allow the drugs to cross the layers of the skin and reach the systemic circulation. Objective: In this study, a new transdermal vehicle was evaluated using progesterone, estradiol, estradiol + estriol (Biest) and ketoprofen administered as model drugs. Methods: To evaluate the ex vivo permeation of the drugs, the Franz vertical diffusion cell with human skin was used. Results: After 24 h, the vehicle was able to deliver 18.32 µg/cm2 of progesterone and 92.07 µg/cm2 of ketoprofen through the skin to the receptor medium. The permeation percentages were 91%, 78.8%, 48.5%, 73.2%, and 63.6%, respectively, for estradiol, estradiol (Biest), estriol (Biest), progesterone and ketoprofen. For all drugs, sufficient amounts were delivered to achieve a systemic effect, and it was also possible to decrease the amount of emulsion applied. Thus, the vehicle demonstrated a high performance and the possibility of it being used for drugs that present difficulties in regards to administration by the transdermal route.

Resveratrol is a phenolic compound that has been widely studied in the last years because of its extensive pharmacological properties. It also has physicochemical properties that are adequate for diffusion through the human skin. An analytical method by high performance liquid chromatography was developed and validated for its determination in transdermal emulsion, as well in receptor media and skin layers. The trans-resveratrol release kinetic followed the Higushi's model (R(2) = 0.9926) with steady-state diffusion flux and lag time of 138.5 µg cm(-2) h(-1) and 0.49 h, respectively. It showed a percentage at 64.96 % for permeation. Thus, the results suggest that the emulsion studied is a potential vehicle for transresveratrol administration by transdermal route.

Background Taxifolin (TAX) is a flavonoid that has numerous pharmacological properties, including an antioxidant ability superior to that of other flavonoids due to its particular structure. Nevertheless, it has low oral bioavailability, which limits its therapeutic application. In this context, potentially important approaches for systemic drug delivery could be by alternative routes such as skin and vaginal mucosa, once both routes have a variety of advantages compared with the oral route, including the ability to bypass both first-pass hepatic metabolism and the consequent degradation in the gastrointestinal tract. Vaginal delivery could also account for a local effect, or an effect on circumvent microregion. Objective The major objective of this study was to develop and validate a high-performance liquid chromatography (HPLC) method for the determination of TAX in a semisolid dosage forms and then to evaluate ex vivo permeations across porcine vaginal mucosa and human skin. Methods TAX was incorporated into an oil-in-water emulsion developed previously by our group. Method for quantification was developed and validated using HPLC. Permeation through human skin and vaginal porcine mucosa were conducted in Franz-type cells. Results The method was precise (CV 0.99), specific, and robust. Permeation experiments through porcine vaginal mucosa and human skin presented permeated percentages equal to 87.43% and 48.09% (per dose), respectively. Conclusion The results suggest that, in the matrixes studied, TAX may be able to exert its biological activities systemically when applied by these routes. Furthermore, it exhibits greater permeability potential when administered by intravaginal route.

BACKGROUND Oxandrolone is a potent synthetic testosterone analogue that possesses strong anabolic property and weak androgenic activity. Apart of their clinical implicances, oral oxandrolone can potentially promote several adverse effects. It is known that the transdermal delivery of drugs may represent a means to avoid or minimize oral adverse effects Thus, the objective of this study was to evaluate the permeability of oxandrolone in human skin on a preliminary basis for possible future determination of the transdermal route as an alternative to oral treatments. METHODS We used a percutaneous absorption assay in Franz diffusion cells coupled with freshly excised human skin. The drug release kinetics were determined to predict the efficiency of this alternative route for the drug. RESULTS Nearly 236 μg (86.7%, in terms of applied dose) of the product was prevented to permeate due to the barrier function of the stratum corneum (SC); 21.6% reached the receptor medium (RM), and the remaining 4.3% were quantified within viable layers of the skin (in vivo, dermis is vascularized). The total amount of drug able to exert effect is the sum of the drug quantified within remained skin (RS) and RM: then, a total of 247.6 μg of oxandrolone (25.9% of the applied dose) would be able to permeate through a non damaged skin. The accuracy of the data is demonstrated by the calculated mass balance (average recovery = 112.6%). CONCLUSION Transdermal oxandrolone could be a viable alternative for traditional oral form, once clinical studies are conducted to prove this hypothesis.

Background Resveratrol is a polyphenol that has gained momentum in therapeutics in the last few years. Objective In this study, we hypothesised that resveratrol could act prophylactically and/or treat inflammatory lesions of the oral cavity after being delivered by two different formulations of buccal mucoadhesive tablets (F1 and F2, which differed in terms of viscosity agents used). Methods This hypothesis was assessed through permeation studies, to verify diffusion of the drug through the buccal mucosa using a porcine model to predict human in vivo behaviour. Results F2 (tablet with less viscosity agent) presented better permeation than F1, but the amount of drug that crossed the mucosa was still low compared to the amount retained within it (35.90 µg found in the receptor medium and 15.63 mg quantified within the mucosa). Conclusion This accounted for a local effect rather than a systemic one, which is desirable for local processes, such as oral mucositis, lichen planus, erythema multiforme, nicotinic stomatitis, recurrent aphthous stomatitis, among others. In this sense, resveratrol-loaded mucoadhesive tablets appear to be a prominent alternative to prevent and/or cure inflammatory lesions of the oral cavity.

Background: The transdermal pharmaceutical forms had a limited usage for a long time, for it was believed that the stratum corneum, the outermost layer of epidermis, made it impracticable the permeation of medications through the skin. However, studies exploring this area of research came up and it was discovered that there are strategies to overcome this barrier, for example, creating a transdermal vehicle able to facilitate the drug absorption. Objective: This study aimed to develop a new transdermal vehicle and compare the permeation flux between products compounded with the innovative vehicle and commercial products, using nimesulide and piroxicam, non steroidal anti-inflammatory, as model drugs. Methods: Four different products were evaluated, two of them were the innovative containing the developed vehicle, and the other two were the commercial products, through ex vivo permeation experiment using Franz-type diffusion cell equipment, and as a membrane, human skin. For evaluation of permeated active pharmaceutical ingredients concentrations, we performed quantification from the receptor solution, stratum corneum and viable epidermis + dermis, through high-performance liquid chromatography analyses. Results: The innovative vehicle promoted increased permeation of active pharmaceutical ingredients through the viable epidermis and dermis, when compared to commercial products, but the stratum corrneum continued to keep the highest retention. Conclusion: The innovative vehicle was capable of enhancing the transdermal absorption of active pharmaceutical ingredients from the manipulated formulations, thus, demonstrating the capability thereof to improve the permeability of active pharmaceutical ingredients by transdermal use.