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1.
Sci Rep ; 14(1): 10673, 2024 05 09.
Article in English | MEDLINE | ID: mdl-38724676

ABSTRACT

U.S. immigration discourse has spurred interest in characterizing who illegalized immigrants are or perceived to be. What are the associated visual representations of migrant illegality? Across two studies with undergraduate and online samples (N = 686), we used face-based reverse correlation and similarity sorting to capture and compare mental representations of illegalized immigrants, native-born U.S. citizens, and documented immigrants. Documentation statuses evoked racialized imagery. Immigrant representations were dark-skinned and perceived as non-white, while citizen representations were light-skinned, evaluated positively, and perceived as white. Legality further differentiated immigrant representations: documentation conjured trustworthy representations, illegality conjured threatening representations. Participants spontaneously sorted unlabeled faces by documentation status in a spatial arrangement task. Faces' spatial similarity correlated with their similarity in pixel luminance and "American" ratings, confirming racialized distinctions. Representations of illegalized immigrants were uniquely racialized as dark-skinned un-American threats, reflecting how U.S. imperialism and colorism set conditions of possibility for existing representations of migrant illegalization.


Subject(s)
Racism , Humans , Male , Female , Adult , Racism/psychology , United States , Young Adult , Emigrants and Immigrants/psychology , Emigration and Immigration , Adolescent , Documentation , Face
2.
Perception ; 52(8): 590-607, 2023 Aug.
Article in English | MEDLINE | ID: mdl-37321648

ABSTRACT

Trustworthy-looking faces are also perceived as more attractive, but are there other meaningful cues that contribute to perceived trustworthiness? Using data-driven models, we identify these cues after removing attractiveness cues. In Experiment 1, we show that both judgments of trustworthiness and attractiveness of faces manipulated by a model of perceived trustworthiness change in the same direction. To control for the effect of attractiveness, we build two new models of perceived trustworthiness: a subtraction model, which forces the perceived attractiveness and trustworthiness to be negatively correlated (Experiment 2), and an orthogonal model, which reduces their correlation (Experiment 3). In both experiments, faces manipulated to appear more trustworthy were indeed perceived to be more trustworthy, but not more attractive. Importantly, in both experiments, these faces were also perceived as more approachable and with more positive expressions, as indicated by both judgments and machine learning algorithms. The current studies show that the visual cues used for trustworthiness and attractiveness judgments can be separated, and that apparent approachability and facial emotion are driving trustworthiness judgments and possibly general valence evaluation.


Subject(s)
Social Perception , Trust , Humans , Trust/psychology , Judgment , Emotions , Effect Modifier, Epidemiologic , Facial Expression
3.
Int J Pharm ; 630: 122454, 2023 Jan 05.
Article in English | MEDLINE | ID: mdl-36455755

ABSTRACT

Airborne particulate matter has been designated as a class 1 carcinogen by the World Health Organization. Nitrate is a toxic substance that accounts for a large proportion of particulate matter, and nitrate toxicity has long been reported. In this study, we aimed to optimize the adsorption and removal of particulate matter containing nitrate for effective elimination by the lungs. To this end, particles were designed to optimize the inhalation and removal efficiencies. These particles were prepared as chitosan-based particles containing N-acetylcysteine by using emulsion diffusion methods. Chitosan adsorbs nitrate, while N-acetylcysteine dissolves mucus. This removal mechanism has been found to occur in various in vitro models that mimic respiratory environments and in vivo models. In particular, the removal of exogenous substances, such as particulate matter, by the motility of respiratory cilia through mucolytic effect was investigated. This new approach for the adsorption and elimination of toxic substances entering the lungs represents an alternative defense mechanism against exposure to nitrates from air pollution.


Subject(s)
Air Pollutants , Chitosan , Particulate Matter , Nitrates , Adsorption , Ferrosoferric Oxide , Acetylcysteine
4.
Psychol Sci ; 33(8): 1240-1256, 2022 08.
Article in English | MEDLINE | ID: mdl-35816672

ABSTRACT

Research on face impressions has often focused on a fixed, universal architecture, treating regional variability as noise. Here, we demonstrated a crucial yet neglected role of cultural learning processes in forming face impressions. In Study 1, we found that variability in the structure of adult perceivers' face impressions across 42 world regions (N = 287,178) could be explained by variability in the actual personality structure of people living in those regions. In Study 2, data from 232 world regions (N = 307,136) revealed that adult perceivers use the actual personality structure learned from their local environment to form lay beliefs about personality, and these beliefs in turn support the structure of perceivers' face impressions. Together, these results suggest that people form face impressions on the basis of a conceptual understanding of personality structure that they have come to learn from their regional environment. The findings suggest a need for greater attention to the regional and cultural specificity of face impressions.


Subject(s)
Personality , Social Perception , Adult , Attitude , Humans , Personality Disorders
5.
Cognition ; 217: 104889, 2021 12.
Article in English | MEDLINE | ID: mdl-34464913

ABSTRACT

Recognition of others' identity through facial features is essential in life. Using both correlational and experimental approaches, we examined how person knowledge biases the perception of others' facial identity. When a participant believed any two individuals were more similar in personality, their faces were perceived to be correspondingly more similar (assessed via mousetracking, Study 1). Further, participants' facial representations of target individuals that were believed to have a more similar personality were found to have a greater physical resemblance (assessed via reverse-correlation, Studies 2 and 3). Finally, when participants learned about novel individuals who had a more similar personality, their faces were visually represented more similarly (Study 4). Together, the findings show that the perception of facial identity is driven not only by facial features but also the person knowledge we have learned about others, biasing it toward alternate identities despite the fact that those identities lack any physical resemblance.


Subject(s)
Facial Recognition , Recognition, Psychology , Humans , Knowledge , Perception
6.
Drug Dev Ind Pharm ; 47(5): 685-693, 2021 May.
Article in English | MEDLINE | ID: mdl-33866911

ABSTRACT

As an active pharmaceutical ingredient, dapagliflozin propanediol monohydrate (D-PD) has been used in the solvated form consisting of dapagliflozin compounded with (S)-propylene glycol and monohydrate at a 1:1:1 ratio. However, dapagliflozin propanediol loses the solvent's reduced lattice structure at slightly higher temperatures. Due to its sensitive solid-state stability, the temperature and humidity are strictly controlled during the production and storage of dapagliflozin. Thus, crystalline molecular complexes containing pharmaceutical salts, solvates, monohydrates, and cocrystals have recently been developed as alternative strategies. This study investigated the dapagliflozin free base (D-FB), D-PD, and dapagliflozin l-proline cocrystals (D-LP). Their solid-state behavior was also evaluated in stress stability studies. The compounds were analyzed using scanning electron microscopy (SEM), powder X-ray diffraction (PXRD), thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), Fourier-transform infrared (FT-IR) spectroscopy, dynamic vapor sorption (DVS), and powder rheology testing. In addition, Carr's index, the Hausner ratio, contact angle, and intrinsic dissolution rate were calculated. Dapagliflozin exhibited distinct physical properties depending upon the differences in solid form and also showed significant differences in solid-state behavior in the stress stability test. In conclusion, D-LP was superior to D-FB or D-PD in physicochemical and mechanical properties.


Subject(s)
Glucosides , Benzhydryl Compounds , Calorimetry, Differential Scanning , Powder Diffraction , Solubility , Spectroscopy, Fourier Transform Infrared , X-Ray Diffraction
7.
J Control Release ; 329: 468-481, 2021 01 10.
Article in English | MEDLINE | ID: mdl-32871206

ABSTRACT

The conventional treatment of pulmonary arterial hypertension (PAH) with oral bosentan hydrate has limitations related to the lack of pulmonary selectivity. In this study, we verified the hypothesis of the feasibility of dry powder inhalation of bosentan as an alternative to oral bosentan hydrate for the treatment of PAH. Inhalable bosentan microparticles with the capability of delivery to the peripheral region of the lungs and enhanced bioavailability have been formulated for PAH. The bosentan microparticles were prepared by the co-spray-drying method with bosentan hydrate and mannitol at different weight ratios. The bosentan microparticles were then characterized for their physicochemical properties, in vitro dissolution behavior, and in vitro aerodynamic performance. The in vivo pharmacokinetics and pathological characteristics were evaluated in a monocrotaline-induced rat model of PAH after intratracheal powder administration of bosentan microparticles, in comparison to orally administered bosentan hydrate. The highest performance bosentan microparticles, named SDBM 1:1, had irregular and porous shape. These microparticles had not only the significantly highest aerosol performance (MMAD of 1.91 µm and FPF of 51.68%) in the formulations, but also significantly increased dissolution rate, compared with the raw bosentan hydrate. This treatment to the lungs was also safe, as evidenced by the cytotoxicity assay. Intratracheally administered SDBM 1:1 elicited a significantly higher Cmax and AUC0-t that were over 10 times higher, compared with those of the raw bosentan hydrate administered orally in the same dose. It also exhibited ameliorative effects on monocrotaline-induced pulmonary arterial remodeling, and right ventricular hypertrophy. The survival rate of the group administrated SDBM1:1 intratracheally was 0.92 at the end of study (Positive control and orally administrated groups were 0.58 and 0.38, respectively). In conclusion, SDBM 1:1 showed promising in vitro and in vivo results with the dry powder inhalation. The inhaled bosentan microparticles can be considered as a potential alternative to oral bosentan hydrate for the treatment of PAH.


Subject(s)
Monocrotaline , Pulmonary Arterial Hypertension , Administration, Inhalation , Animals , Bosentan , Dry Powder Inhalers , Particle Size , Rats
8.
J Exp Psychol Hum Percept Perform ; 46(11): 1328-1343, 2020 Nov.
Article in English | MEDLINE | ID: mdl-32757588

ABSTRACT

Women prefer male faces with feminine shape and masculine reflectance. Here, we investigated the conceptual correlates of this preference, showing that it might reflect women's preferences for feminine (vs. masculine) personality in a partner. Young heterosexual women reported their preferences for personality traits in a partner and rated male faces-manipulated on masculinity/femininity-on stereotypically masculine (e.g., dominance) and feminine traits (e.g., warmth). Masculine shape and reflectance increased perceptions of masculine traits but had different effects on perceptions of feminine traits and attractiveness. While masculine shape decreased perceptions of both attractiveness and feminine traits, masculine reflectance increased perceptions of attractiveness and, to a weaker extent, perceptions of feminine traits. These findings are consistent with the idea that sex-dimorphic characteristics elicit personality trait judgments, which might in turn affect attractiveness. Importantly, participants found faces attractive to the extent that these faces elicited their preferred personality traits, regardless of gender typicality of the traits. In sum, women's preferences for male faces are associated with their preferences for personality traits. (PsycInfo Database Record (c) 2020 APA, all rights reserved).


Subject(s)
Choice Behavior/physiology , Facial Recognition/physiology , Femininity , Masculinity , Personality/physiology , Sexual Behavior/physiology , Social Perception , Adult , Female , Humans , Young Adult
9.
Acta Psychol (Amst) ; 203: 103011, 2020 Feb.
Article in English | MEDLINE | ID: mdl-31981825

ABSTRACT

People's ability to learn about the affective value of others is impressive. However, it is unclear whether this learning solely reflects general affect-based processes or a mixture of affect-based and person-attribution processes. Consistent with the former possibility, people's ability to learn the affective value of people and places have been shown to be comparable (Falvello, Vinson, Ferrari, & Todorov, 2015). To investigate whether general affect-based processes are sufficient to account for this kind of learning, we presented participants with images paired with valenced statements that were either relevant (e.g., a person statement with a person image) or irrelevant (e.g., a person statement with a non-person image). After this presentation, participants evaluated the goodness or badness of the images. In Experiment 1, we found that the learning effects for faces and places were comparable and occurred only when the statements were relevant. However, when we presented the images with multiple statements of the same valence (Experiments 2-4), we found that places acquired affective value from both relevant and irrelevant statements. In contrast, faces were less likely to acquire affective value from irrelevant statements. Our findings suggest that although general affect-based processes might be sufficient to account for affective learning of places, affective learning of faces might involve both affect-based and person-attribution processes.


Subject(s)
Affect/physiology , Association Learning/physiology , Adult , Attention/physiology , Conditioning, Psychological/physiology , Facial Expression , Female , Humans , Male , Psychomotor Performance/physiology , Reaction Time/physiology , Young Adult
10.
J Exp Psychol Gen ; 149(2): 323-342, 2020 Feb.
Article in English | MEDLINE | ID: mdl-31294585

ABSTRACT

Trustworthiness and dominance impressions summarize trait judgments from faces. Judgments on these key traits are negatively correlated to each other in impressions of female faces, implying less differentiated impressions of female faces. Here we test whether this is true across many trait judgments and whether less differentiated impressions of female faces originate in different facial information used for male and female impressions or different evaluation of the same information. Using multidimensional rating datasets and data-driven modeling, we show that (a) impressions of women are less differentiated and more valence-laden than impressions of men and find that (b) these impressions are based on similar visual information across face genders. Female face impressions were more highly intercorrelated and were better explained by valence (Study 1). These intercorrelations were higher when raters more strongly endorsed gender stereotypes. Despite the gender difference, male and female impression models-derived from separate trustworthiness and dominance ratings of male and female faces-were similar to each other (Study 2). Further, both male and female models could manipulate impressions of faces of both genders (Study 3). The results highlight the high-level, evaluative effect of face gender in impression formation-women are judged negatively to the extent their looks do not conform to expectations, not because people use different facial information across genders but because people evaluate the information differently across genders. (PsycINFO Database Record (c) 2020 APA, all rights reserved).


Subject(s)
Attitude , Facial Expression , Judgment , Sexism/psychology , Sexism/statistics & numerical data , Social Perception , Adult , Computer Simulation , Female , Humans , Male , Students/psychology , Students/statistics & numerical data , Young Adult
11.
Nat Hum Behav ; 4(3): 287-293, 2020 03.
Article in English | MEDLINE | ID: mdl-31819209

ABSTRACT

Impressions of competence from faces predict important real-world outcomes, including electoral success and chief executive officer selection. Presumed competence is associated with social status. Here we show that subtle economic status cues in clothes affect perceived competence from faces. In nine studies, people rated the competence of faces presented in frontal headshots. Faces were shown with different upper-body clothing rated by independent judges as looking 'richer' or 'poorer', although not notably perceived as such when explicitly described. The same face when seen with 'richer' clothes was judged significantly more competent than with 'poorer' clothes. The effect persisted even when perceivers were exposed to the stimuli briefly (129 ms), warned that clothing cues are non-informative and instructed to ignore the clothes (in one study, with considerable incentives). These findings demonstrate the uncontrollable effect of economic status cues on person perception. They add yet another hurdle to the challenges faced by low-status individuals.


Subject(s)
Clothing , Economic Status , Facial Recognition , Social Perception , Adult , Cues , Female , Humans , Male , Young Adult
12.
Vision Res ; 165: 131-142, 2019 12.
Article in English | MEDLINE | ID: mdl-31734634

ABSTRACT

Face perception is based on both shape and reflectance information. However, we know little about the relative contribution of these kinds of information to social judgments of faces. In Experiment 1, we generated faces using validated computational models of attractiveness, competence, dominance, extroversion, and trustworthiness. Faces were manipulated orthogonally on five levels of shape and reflectance for each model. Both kinds of information had linear and additive effects on participants' social judgments. Shape information was more predictive of dominance, extroversion, and trustworthiness judgments, whereas reflectance information was more predictive of competence judgments. In Experiment 2, to test whether the amount of visual information alters the relative contribution of shape and reflectance information, we presented faces - varied on attractiveness, competence, and dominance - for five different durations (33-500 ms). For all judgments, the linear effect of both shape and reflectance increased as duration increased. Importantly, the relative contribution did not change across durations. These findings show that that the judged dimension is critical for which kind of information is weighted more heavily in judgments and that the relative contribution of shape and reflectance is stable across the amount of visual information available.


Subject(s)
Facial Expression , Facial Recognition/physiology , Judgment/physiology , Social Perception , Adult , Humans , Male
13.
Int J Nanomedicine ; 14: 5381-5396, 2019.
Article in English | MEDLINE | ID: mdl-31409994

ABSTRACT

Background: Tacrolimus (TCR), also known as FK-506, is a biopharmaceutics classification system (BCS) class II drug that is insoluble in water because of its high log P values. After dermal application, TCR remains in the stratum corneum and passes through the skin layers with difficulty. Purpose: The objectives of this study were to develop and evaluate solid lipid nanoparticles (SLNs) with thermosensitive properties to improve penetration and retention. Methods: We prepared TCR-loaded thermosensitive solid lipid nanoparticles (TCR-SLNs) with different types of surfactants on the shell of the particle, which conferred the advantages of enhancing skin permeation and distribution. We also characterized them from a physic point of view and performed in vitro and in vivo evaluations. Results: The TCR contained in the prepared TCR-SLN was in an amorphous state and entrapped in the particles with a high loading efficiency. The assessment of ex vivo skin penetration using excised rat dorsal skin showed that the TCR-SLNs penetrated to a deeper layer than the reference product (0.1% Protopic®). In addition, the in vivo skin penetration test demonstrated that TCR-SLNs delivered more drug into deeper skin layers than the reference product. FT-IR images also confirmed drug distribution of TCR-SLNs into deeper layers of the skin. Conclusion: These results revealed the potential application of thermosensitive SLNs for the delivery of difficult-to-permeate, poorly water-soluble drugs into deep skin layers.


Subject(s)
Dermis/metabolism , Lipids/chemistry , Nanoparticles/chemistry , Tacrolimus/pharmacology , Temperature , Administration, Cutaneous , Animals , Calorimetry, Differential Scanning , Dermis/drug effects , Drug Liberation , Irritants/toxicity , Nanoparticles/ultrastructure , Particle Size , Rabbits , Rats, Sprague-Dawley , Skin Absorption/drug effects , Skin Tests , Spectroscopy, Fourier Transform Infrared , Surface-Active Agents/chemistry , X-Ray Diffraction
14.
Materials (Basel) ; 12(6)2019 Mar 26.
Article in English | MEDLINE | ID: mdl-30917621

ABSTRACT

Lacosamide (LCM) is a third-generation antiepileptic drug. Selective action of the drug on voltage-gated sodium channels reduces side effects. Oral administration of LCM shows good pharmacokinetic profile. However, the bitter taste of LCM is a barrier to the development of oral formulations. In this study, we aimed to prepare encapsulated LCM microparticles (MPs) for masking its bitter taste. Encapsulated LCM MPs were prepared with Eudragit® E100 (E100), a pH-dependent polymer, by spray drying. Three formulations comprising different ratios of LCM and E100 (3:1, 1:1, and 1:3) were prepared. Physicochemical tests showed that LCM was in an amorphous state in the prepared formulations, and they were not miscible. LCM-E100 (1:3) had a rough surface due to surface enrichment of LCM. Increased E100 ratio in LCM-E100 MPs resulted in better taste-making effectiveness: LCM-E100 (1:1) and LCM-E100 (1:3) showed good taste-masking effectiveness, while LCM-E100 (3:1) could not mask the bitter taste of LCM. Dissolution results of the prepared formulations showed good correlation with taste-masking effectiveness. Nevertheless, high E100 ratio reduced the stability of the prepared formulations. Especially the difference in initial dissolution profile observed for LCM-E100 (1:3) indicated rapid reduction in taste-masking effectiveness and surface recrystallization. Therefore, LCM-E100 formulation in the ratio of 1:1 was selected as the best formulation with good taste-masking effectiveness and stability.

15.
Psychol Sci ; 30(1): 65-79, 2019 01.
Article in English | MEDLINE | ID: mdl-30526301

ABSTRACT

Competence impressions from faces affect important decisions, such as hiring and voting. Here, using data-driven computational models, we identified the components of the competence stereotype. Faces manipulated by a competence model varied in attractiveness (Experiment 1a). However, faces could be manipulated on perceived competence controlling for attractiveness (Experiment 1b); moreover, faces perceived as more competent but not attractive were also perceived as more confident and masculine, suggesting a bias to perceive male faces as more competent than female faces (Experiment 2). Correspondingly, faces manipulated to appear competent but not attractive were more likely to be classified as male (Experiment 3). When masculinity cues that induced competence impressions were applied to real-life images, these cues were more effective on male faces (Experiment 4). These findings suggest that the main components of competence impressions are attractiveness, confidence, and masculinity, and they reveal gender biases in how we form important impressions of other people.


Subject(s)
Beauty , Facial Recognition/physiology , Femininity , Masculinity , Sexism , Social Perception , Stereotyping , Adult , Female , Humans , Male , Middle Aged , Young Adult
16.
Drug Des Devel Ther ; 12: 711-719, 2018.
Article in English | MEDLINE | ID: mdl-29670329

ABSTRACT

BACKGROUND: Norquetiapine (N-desalkyl quetiapine, NQ) is an active metabolite of quetiapine with stable pharmacokinetic and pharmacological properties. However, its short half-life is a drawback for clinical applications, and long-acting formulations are required. PURPOSE: The objectives of this study were to prepare improved entrapment efficiency NQ freebase microspheres by the solvent evaporation method with poly(d,l-lactic-co-glycolic acid) (PLGA) as a release modulator and to evaluate their physicochemical and in vitro/in vivo release properties. METHODS: NQ freebase PLGA (1:5 w/w) formulations were prepared by the oil-in-water (o/w) emulsion-solvent evaporation method. A solution of the drug and PLGA in 9:1 v/v dichloromethane:ethanol was mixed with 0.2% polyvinyl alcohol and homogenized at 2,800 rpm. The emulsion was stirred for 3 h to dilute and evaporate the solvent. After that, the resulting product was freeze-dried. Drug-loading capacity was measured by the validated RP-HPLC method. The surface morphology of the microspheres was observed by scanning electron microscopy (SEM), and the physicochemical properties were evaluated by differential scanning calorimetry, powder X-ray diffraction, and Fourier-transform infrared spectroscopy particle size distribution. The in vitro dissolution test was performed using a rotary shaking bath at 37°C, with constant shaking at 50 rpm in sink condition. RESULTS: The NQ freebase microspheres prepared by o/w emulsion-solvent evaporation showed over 30% efficiency. NQ was confirmed to be amorphous in the microspheres by powder X-ray diffraction and differential scanning calorimetry. Special chemical interaction in the microspheres was not observed by FT-IR. The in vitro dissolution test demonstrated that the prepared microspheres' release properties were maintained for more than 20 days. The in vivo test also confirmed that the particles' long acting properties were maintained. Therefore, good in vitro-in vivo correlation was established. CONCLUSION: In this study, NQ freebase-PLGA microspheres showed potential for the treatment of schizophrenia for long-periods.


Subject(s)
Dibenzothiazepines/pharmacokinetics , Lactic Acid/pharmacokinetics , Microspheres , Polyglycolic Acid/pharmacokinetics , Animals , Dibenzothiazepines/administration & dosage , Dibenzothiazepines/chemistry , Lactic Acid/administration & dosage , Lactic Acid/chemistry , Particle Size , Polyglycolic Acid/administration & dosage , Polyglycolic Acid/chemistry , Polylactic Acid-Polyglycolic Acid Copolymer , Rats , Rats, Sprague-Dawley , Spectroscopy, Fourier Transform Infrared , Surface Properties
17.
Arch Pharm Res ; 40(8): 943-951, 2017 Aug.
Article in English | MEDLINE | ID: mdl-28770536

ABSTRACT

Minoxidil is widely used for treatment of androgenic alopecia. Commercial products containing minoxidil are usually in solution form. Repeated applications of minoxidil solution can lead to adverse effects such as skin irritation and horniness. The aims of this study were to prepare lecithin-based microparticle in minoxidil solution for enhancement of minoxidil topical delivery and skin protection and evaluate the ability of lecithin on in vitro delivery, in vivo hair growth, and skin trouble improvement compared to commercial minoxidil solution. In in vitro skin permeation study, minoxidil solution containing lecithin microparticle showed higher skin penetration rate and higher retention of drug inside the skin compared to minoxidil solution without lecithin. After topical application of minoxidil solutions with or without lecithin to C57BL/6 mice, minoxidil 5% solution containing lecithin microparticle showed hair re-growth as efficient as commercial product of minoxidil 5% solution. It also significantly improved skin troubles while commercial product presented horny substance and crust formation. Therefore, the lecithin-based microparticle in minoxidil 5% solution has good ability to promote hair growth without adverse effects.


Subject(s)
Drug Delivery Systems , Hair/drug effects , Lecithins/chemistry , Minoxidil/administration & dosage , Administration, Cutaneous , Alopecia/drug therapy , Animals , Drug Carriers/chemistry , Female , Hair/growth & development , Humans , Male , Mice , Mice, Inbred C57BL , Microspheres , Minoxidil/pharmacokinetics , Minoxidil/pharmacology , Pharmaceutical Solutions , Rats , Rats, Sprague-Dawley , Skin Absorption , Vasodilator Agents/administration & dosage , Vasodilator Agents/pharmacokinetics , Vasodilator Agents/pharmacology
18.
Drug Deliv ; 24(1): 1056-1066, 2017 Nov.
Article in English | MEDLINE | ID: mdl-28687046

ABSTRACT

The film forming gel, adhered to skin surfaces upon application and formed a film, has an advantage onto skin to provide protection and continuous drug release to the application site. This study aimed to prepare a chitosan-based film forming gel containing ketoprofen (CbFG) and to evaluate the CbFG and film from CbFG (CbFG-film). CbFG were prepared with chitosan, lactic acid and various skin permeation enhancers. The physicochemical characteristics were evaluated by texture analysis, viscometry, SEM, DSC, XRD and FT-IR. To identify the mechanism of skin permeation, in vitro skin permeation study was conducted with a Franz diffusion cell and excised SD-rat and hairless mouse dorsal skin. In vivo efficacy assessment in mono-iodoacetate (MIA)-induced rheumatoid arthritis animal model was also conducted. CbFG was successfully prepared and, after applying CbFG to the excised rat dorsal skin, the CbFG-film was also formed well. The physicochemical characteristics of CbFG and CbFG-film could be explained by the grafting of oleic acid onto chitosan in the absence of catalysts. In addition, CbFG containing oleic acid had a higher skin permeation rate in comparison with any other candidate enhancers. The in vivo efficacy study also confirmed significant anti-inflammatory and analgesic effects. Consequently, we report the successful preparation of chitosan-based film forming gel containing ketoprofen with excellent mechanical properties, skin permeation and anti-inflammatory and analgesic effects.


Subject(s)
Chitosan/chemistry , Administration, Cutaneous , Animals , Anti-Inflammatory Agents, Non-Steroidal , Gels , Ketoprofen , Mice , Rats , Skin , Skin Absorption , Spectroscopy, Fourier Transform Infrared
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