Enhanced stability of phenylethyl resorcinol in elastic vesicular formulations

Purpose: To enhance the stability and reduce photo-degradation of phenylethyl resorcinol (PR) by elastic vesicle formation.Methods: PR solution was stored at different temperatures, pH conditions, and under protected and unprotected natural light. The color of the solution and total active content were investigated. Three types of elastic vesicles, viz, ethosomes, transfersomes and invasomes, were prepared and their sedimentation in formulations and total active content were investigated before and after storage under various conditions for 4 months. The stability of the solutions and vesicular formulations were assessed.Results: PR solution was unstable at pH 9, higher temperature (70 ± 1 oC) and under natural light. The color of PR solution changed from colorless to orange tone and the PR content decreased. On the other hand, PR entrapped within ethosome, tranfersome and invasome vesicles showed better stability, color change was not observed in the formulations, and PR content remained > 90 %.Conclusion: All the vesicles display reduced degradation of PR under thermal and natural light. Thus, PR vesicular formulation enhances stability and improves the quality of the product for use in topical administration.Keywords: Phenylethyl resorcinol, Degradation, Ethosomes, Transfersomes, Invasomes, Topical administratio

Bacterial Cellulose-Carboxymethyl Cellulose (BC:CMC) dry formulation as stabilizer and texturizing agent for surfactant-free cosmetic formulations

Generic cosmetic creams (oil-in-water emulsions) were prepared using dry Bacterial Cellulose and Carboxymethyl Cellulose (BC:CMC) to study the possibility of partially or completely replacing surfactants, while ensuring a long-term stability and the required organoleptic characteristics. BC:CMC was benchmarked against two hydrocolloidal Avicel products (PC-591 and PC-611), commonly used as thickeners and stabilizing aids in cosmetics production. The emulsions were then characterized regarding storage stability, rheology, texture and microscopic features. The full replacement of 5.5% surfactants with only 0.75% BC:CMC consistently showed similar results to those obtained with surfactants, namely concerning viscosity and texture. Although producing emulsions with larger oil droplets, BC:CMC provided for a very effective stabilization through a Pickering effect and by structuring the continuous phase. The more effective Avicel tested (PC-591) required a higher concentration (1.5 %) to achieve similar rheological profile but was ineffective in stabilizing the oil phase in a surfactant-free formulation with the adopted protocol. By replacing surfactants, dry BC:CMC matches a strong market need since both end users and manufacturers increasingly seek natural ingredients for cosmetic formulations.This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UIDB/ 04469/2020 unit and BioTecNorte operation (NORTE-01-0145-FEDER 000004) funded by the European Regional Development Fund under the scope of Norte2020 - Programa Operacional Regional do Norte. Daniela Martins also gratefully acknowledges FCT for the PhD scholarship, reference SFRH/BD/115917/2016.info:eu-repo/semantics/publishedVersio

Dizajniranje i vrednovanje bioadhezijskog filma za transdermalnu isporuku propranolol hidroklorida

The objective of the study was to develop a suitable transdermal delivery system for propranolol hydrochloride (PPL) via employing chitosan as a film former. Drug concentration uniformity, thickness, moisture uptake capacity and skin bioadhesion of the films were characterized. The effects of chitosan and PPL concentration and different penetration enhancers on the release and permeation profiles from the films were investigated. Skin irritation of the candidate film was evaluated. Chitosan film (PPL 2 mg cm2, chitosan 2 % m/m, cineol 10 %, m/m) was found non-irritant and achieved 88.2 % release after 8 hours in phosphate buffer. Significant high (p < 0.001) permeation of PPL through rat skin was obtained using this film compared to the film without enhancer (about 8 times enhancement factor), making it a promising transdermal delivery system for PPL.Cilj rada bio je razvoj pogodnog transdermalnog sustava na bazi kitozana za isporuku propranolol hidroklorida (PPL). Svim pripravcima ispitana je jednoličnost udjela lijeka, debljina, sposobnost vlaženja i bioadhezivnost na kožu. Ispitivan je i utjecaj kitozana, koncentracije PPL-a i sredstva za povećanje permeacije na oslobađanje i permeacijski profil, te potencijalni iritacijski učinak na kožu. Iz kitozanskog filma (PPL 2 mg cm2, 2 %, m/m, kitozana i 10 %, m/m, cineola), koji nije djelovao iritabilno, postignuto je 88,2 % oslobađanja nakon 8 sati u fosfatnom puferu. S ovim pripravkom postignuta je i vrlo značajna (p < 0,001) permeacija PPL kroz kožu štakora, oko osam puta veća u usporedbi s filmom bez sredstva za povećanje permeacije. Pripravak bi se mogao upotrijebiti za transdermalnu isporuku PPL

Enhancement of Mycophenolate Mofetil Permeation for Topical Use by Eucalyptol and N-Methyl-2-pyrrolidone

Mycophenolate mofetil (MMF) is a prodrug of mycophenolic acid (MPA) which can be metabolized by esterase. MMF has been approved by the United States Food and Drug Administration (USFDA) for treatment of psoriasis patient with skin symptoms. However, it remains unclear whether MMF is efficiently effective to treat skin symptoms developed from psoriasis. The insufficient amount of MMF penetrating through the skin results in the treatment failure due to the difficulty in MMF penetration through the stratum corneum. Skin permeation enhancers such as eucalyptol (EUL) and N-methyl-2-pyrrolidone (NMP) potentially aid in increasing skin penetration. This study aimed to investigate the effects of a concentration ratio (% w/v) between two enhancers (EUL and NMP). The results showed that EUL enhanced MMF permeation with an enhancement ratio (ER) of 3.44 while NMP was not able to promote the penetration of MMF. Interestingly, the synergistic effect of the two enhancers was observed with a suitable ratio given that the ER was 8.21. EUL and NMP are promising enhancers for the development of MMF based skin product

Hydrolyzed Fish Collagen Serum from By-Product of Food Industry: Cosmetic Product Formulation and Facial Skin Evaluation

Fish collagen is a good source of protein and essential amino acids. It has a wide range of applications in food manufacturing, pharmaceutics, cosmetics, etc. By-products obtained from fish processing industries are currently used as alternative sources for the production of collagen and gelatin. Hydrolyzed collagen derived from fish skin has properties that are beneficial in cosmetic products. The aim of this study was to: (1) formulate a cosmetic product containing hydrolyzed fish collagen obtained from a by-product of fish processing industries, and other effective ingredients such as vitamin C, vitamin E and vitamin B3, (2) evaluate the physicochemical properties and stability of the product, and (3) conduct a facial skin evaluation test wherein volunteers use the product and have their facial skin analyzed. The formulated serum was translucent with low turbidity and had a pH of 7.7, and a viscosity of 1333 cps. The stability of the formulation was good, without any significant change in appearance, pH and viscosity as tested by freeze–thaw cycle testing, and after storage at room temperature for a period of 6 months. Furthermore, the results from the Visia skin analysis instrument revealed that the product was able to enhance facial skin moisture, reduce skin pores and wrinkles, and brighten the skin significantly when regularly used for at least 2 weeks. In conclusion, it was observed that hydrolyzed fish collagen obtained from a by-product of fish processing industries could be a sustainable and suitable material utilized in the production of safe and useful cosmeceutical products

Liposomal Encapsulated Rhodomyrtone: A Novel Antiacne Drug

Rhodomyrtone isolated from the leaves of Rhodomyrtus tomentosa possesses antibacterial, anti-inflammatory, and anti-oxidant activities. Since rhodomyrtone is insoluble in water, it is rather difficult to get to the target sites in human body. Liposome exhibited ability to entrap both hydrophilic and hydrophobic compounds and easily penetrate to the target site. The present study aimed to develop a novel liposomal encapsulated rhodomyrtone formulations. In addition, characterization of liposome, stability profiles, and their antiacne activity were performed. Three different formulations of total lipid concentrations 60, 80, and 100 μmol/mL were used. Formulation with 60 μmol/mL total lipid (phosphatidylcholine from soybean and cholesterol from lanolin in 4 : 1, w/w) exhibited the highest rhodomyrtone encapsulation efficacy (65.47 ± 1.7%), average particle size (209.56 ± 4.8 nm), and ζ-potential (–41.19 ± 1.3 mV). All formulations demonstrated good stability when stored for 2 months in dark at 4°C as well as room temperature. Minimal inhibitory concentration and minimal bactericidal concentration values of liposomal formulation against 11 clinical bacterial isolates and reference strains ranged from 1 to 4 and from 4 to 64 μg/mL, respectively, while those of rhodomyrtone were 0.25–1 and 0.5–2 μg/mL, respectively. The MIC and MBC values of liposome formulation were more effective than topical drugs against Staphylococcus aureus and Staphylococcus epidermidis