November 2023
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10 Reads
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1 Citation
Journal of Pharmaceutical and Biomedical Analysis
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November 2023
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10 Reads
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1 Citation
Journal of Pharmaceutical and Biomedical Analysis
October 2019
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118 Reads
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12 Citations
Recent Patents on Drug Delivery & Formulation
Background The human nail is a unique barrier with keratinized constitution that favors protection and fine touch. However, many disorders can affect the nail, among them are the onychomycosis and psoriasis. Systemic oral therapy has been applied to treat these diseases, even presenting disadvantages including side effects, drug interactions, contraindications, toxicity, high cost and low patient compliance. A great option to succeed in dealing with the problems associated to oral therapy is the topical administration of drugs. However, nail composition, low diffusion through ungual route and reduced tissue bioavailability for topical treatments are limiting factors. These drawbacks can be overcome by promoting penetration through the nails by employing penetration enhancers. Objective The review focuses on patents that highlight permeation enhancers applied to nail drug delivery to the treatment of onychomycosis and psoriasis. Methods Literature and patent searches were conduced regarding the topic of interest. Results The substantial literature and patent search revealed that permeation enhancers, especially chemicals, are great strategies for promoting ungual delivery of drugs. Conclusion Nail topical therapy containing permeation enhancers is an attractive option to delivering localized treatments.
September 2019
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479 Reads
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8 Citations
Arabian Journal of Chemistry
Ketoprofen is a non-steroidal anti-inflammatory drug (NSAID) widely used to treat rheumatoid arthritis and other inflammatory diseases. Normally used by oral route, this drug presents numerous side effects related to this administration route, such as nausea, dyspepsia, diarrhea, constipation and even renal complications. To avoid that, topical administration of ketoprofen represents a good alternative, since this drug has both partition coefficient and aqueous solubility suitable for skin application, compared to other NSAIDs. In this study, we describe the production of a nanoemulsion containing ketoprofen, its skin permeation and in vitro release study and a novel validation method to analyze this drug in the permeation samples and a forced degradation study using skin and nanoemulsion samples. The new HPLC method was validated, with all specifications in accordance with validation parameters and with an easy chromatographic condition. Forced degradation study revealed that ketoprofen is sensitive to acid and basic hydrolysis, developing degradation peaks after exposure to these factors. Concerning in vitro release from the nanoemulsion, release curves presented first order profile and were not similar to each other. After 8 h, 85% of ketoprofen was release from the nanoemulsion matrix while 49% was release from control group. In skin permeation study, nanoemulsion enabled ketoprofen to pass through the skin and enhanced retention in the epidermis and stratum corneum, layer on which the formulation presented statistically different values compared to the control group. Keywords: Validation, Forced degradation, Nanoemulsion
April 2019
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1,173 Reads
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113 Citations
Biomolecules
Essential oils are natural products with a complex composition. Terpenes are the most common class of chemical compounds present in essential oils. Terpenes and the essential oils containing them are widely used and investigated by their pharmacological properties and permeation-enhancing ability. However, many terpenes and essential oils are sensitive to environmental conditions, undergoing volatilization and chemical degradation. In order to overcome the chemical instability of some isolated terpenes and essential oils, the encapsulation of these compounds in nanostructured systems (polymeric, lipidic, or molecular complexes) has been employed. In addition, nanoencapsulation can be of interest for pharmaceutical applications due to its capacity to improve the bioavailability and allow the controlled release of drugs. Topical drug administration is a convenient and non-invasive administration route for both local and systemic drug delivery. The present review focuses on describing the current status of research concerning nanostructured delivery systems containing isolated terpenes and/or essential oils designed for topical administration and on discussing the use of terpenes and essential oils either for their biological activities or as permeation enhancers in pharmaceutic formulations.
November 2018
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62 Reads
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79 Citations
Talanta
Essential oils are natural products extracted from plants that present volatile and thermolabile characteristics. Essential oils have become products of interest in many fields, including the pharmaceutical, due to their medicinal properties. In recent years, the interest in the encapsulation of essential oils in nanometric systems for therapeutic approaches has risen and a number of studies have been published. This review intended to set a panorama on the research within this field through a data survey and identify the organic nanostructured systems, the preparation techniques and analytical quantification methods employed. Many techniques used to prepare nanosystems loaded with essential oils involve heating or solvent evaporation steps that may damage their composition. In this context, the quantification of essential oil on the final nanosystems is impaired. However, in more than half of the research papers, the quantification is ignored or an indirect quantification is performed, assuming no volatilisation upon formulation processes. Analytical methods used to assess essential oil encapsulation efficiency were discussed regarding their suitability.
August 2017
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145 Reads
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51 Citations
AAPS PharmSciTech
Copaiba oil is used as a popular medicine in the Amazonian forest region, especially due to its anti-inflammatory properties. In this paper, we describe the formulation of hydrogel containing copaiba oil nanoemulsions (with positive and negative charges), its skin permeation, and its anti-inflammatory activity in two in vivo models: mouse ear edema and rat paw edema. Three hydrogels were tested (Carbopol(®), hydroxyethylcellulose and chitosan), but only Carbopol(®) and hydroxyethylcellulose hydrogels presented good stability and did not interfere with the nanoemulsions droplet size and polydispersity index. In skin permeation assay, both formulations, positively charged nanoemulsion (PCN) and negatively charged nanoemulsion (NCN), presented a high retention in epidermis (9.76 ± 2.65 μg/g and 7.91 ± 2.46 μg/cm(2), respectively) followed by a smaller retention in the dermis (2.43 ± 0.91 and 1.95 ± 0.56 μg/cm(2), respectively). They also presented permeation to the receptor fluid (0.67 ± 0.22 and 1.80 ± 0.85 μg/cm(2), respectively). In addition, anti-inflammatory effect was observed to NCN and PCN with edema inhibitions of 69 and 67% in mouse ear edema and 32 and 72% in rat paw edema, respectively. Histological cuts showed the decrease of inflammatory factors, such as dermis and epidermis hyperplasia and inflammatory cells infiltration, confirming the anti-inflammatory effect from both copaiba oil nanoemulsions incorporated in hydrogel.
February 2015
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612 Reads
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58 Citations
Journal of Pharmaceutical and Biomedical Analysis
Copaiba oil is largely used in the Amazonian region for the treatment of inflammation, and recent studies demonstrated that one of the major components of the oil, β-caryophyllene (CAR), is a potent anti-inflammatory. The nanoemulsification of this oleoresin, which has unctuous character, converts it in a more acceptable hydrophilic formulation and may improve CAR penetration through the skin due to the small droplet size and the high contact surface afforded by the nanoemulsions. This paper describes the validation of a novel, sensitive, practical and solvent free method that uses gas chromatography in headspace mode coupled with mass spectrometry to evaluate the skin permeation/retention of CAR from the crude copaiba oil and its nanoemulsion. Our results show that the bioanalytic method was fully validated, demonstrating linearity (r2 > 0.99), specificity (no peaks co-eluting with CAR retention time), precision (RSD < 15%) and accuracy (recovery > 90%) within the accepted parameters and that the copaiba oil nanoemulsion presented a better skin penetration compared to the crude oil, with CAR achieving the most profound layer of the skin, the dermis.
... Although ME could not be detected in the receptor fluid, NP reached this compartment in the order of 441.1 ± 92.1 µg/cm 2 . This interesting result indicates that NP has the potential to completely cross all nail plate layers and reach the nail bed, which is the site of infection of some subtypes of this disease [19]. Thus, its permeation properties allow NP to be studied in several other biological models where the difficult task of reaching the infection target is a necessity. ...
November 2023
Journal of Pharmaceutical and Biomedical Analysis
... The combination of chemical enhancers and iontophoresis also yielded synergetic drug transport [24,51]. Five well-known permeation enhancers were selected as these chemical agents have demonstrated their potential to enhance nail drug permeation in various studies [24,52]. The amount of efinaconazole loaded into the nail with various enhancers tested is presented in Figure 2b. ...
October 2019
Recent Patents on Drug Delivery & Formulation
... Ketoprofen content was determined using a Shimadzu system (CBM-20 A, SIL-20A, LC-20AT, DGU-20A S, CTO-10AS VP) using a UV/Vis detector (SPD-20 A, Shimadzu, Kyōto, Japan) with a reverse-phase C 18 column (EC 125/4 NUCLEOSIL 100-5 C18, Macherey-Nagel GmbH & Co. KG, Dueren, Germany). Measurements were conducted based on a previously described method with an injection volume of 20 µl at a temperature of 35 • C with the UV detector set to 254 nm and a mobile phase of methanol and 0.1 % trifluoroacetic acid (60:40) set to a flow rate of 1 ml/min (Lucca, 2020). Calibration was done in two ranges; from 0.0002 mg/ml to 0.01 mg/ml and from 0.01 mg/ml to 0.1 mg/ml with coefficients of correlation (r 2 ) of 0.969 and 0.997 respectively. ...
September 2019
Arabian Journal of Chemistry
... 40,41 This hydrophobic nature of limonene may play a crucial role in specic catalytic reactions where interaction with hydrophilic surfaces might not be favored. 42,43 Characterization ...
April 2019
Biomolecules
... 15 Extraction and quantification of the real OE content is necessary, and studies that quantify the real OE content by spectrophotometry do not consider the possible interferences of nanocapsule components, since their studies do not cite the validation of the method used. 22 On this premise, the present proposal to use derivative spectrophotometry, to determine the real OE value in nanocapsule powder, arises from the observation of the interference that the matrix exerted on the absorbance spectra in OE solutions (Figure 1), which makes it impossible direct application of spectrophotometry. Thus, in order to circumvent Braz. ...
November 2018
Talanta
... Lawsonia inermis ethanolic extract enriched in terpenoids, alkaloids, tannins, and saponins was loaded in chitosan/PVA hydrogels [94] with a slow release of about 50% of the drugs, highlighting interesting wound healing properties. Essential oils from copaiba rich in β-caryophyllene [95], along with those produced from Eucalyptus, Ginger, and Cumin that contain tannins, phenols, and terpenoids [96,97], were loaded in chitosan-based hydrogels, highlighting an acceleration in wound healing and optimal antibacterial and anti-inflammatory effects. Bee honey, rich in phenols and enzymes, was incorporated into a chitosan-based hydrogel allowing for the maintenance of a well-structured epidermis and accelerating wound healing [98]. ...
August 2017
AAPS PharmSciTech
... These results indicate that both monoterpenes had minimal permeation through the skin, with myrcene showing significantly lower permeation than cymene ( Figure 2C. The low permeation rates benefit repellent formulations as they minimize systemic absorption and potential toxicity [14,42,43]. ...
February 2015
Journal of Pharmaceutical and Biomedical Analysis