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3.
Sci Rep ; 12(1): 13102, 2022 07 30.
Artigo em Inglês | MEDLINE | ID: mdl-35907916

RESUMO

A shift towards natural anti-aging ingredients has spurred the research to valorize traditionally used plants. In this context, Rosmarinus officinalis L. was evaluated for its photoprotective, antioxidant, anti-inflammatory, and anti-wrinkling properties. GC/MS and LC-ESI-HRMS based phytochemical profiling of rosemary leaves hexane extract resulted in the identification of 47 and 31 compounds, respectively and revealed rich content in triterpenoids, monoterpenoids and phenolic diterpenes. In vitro assays confirmed the antioxidant, anti-aging, and wound healing potential of rosemary extract along with a good safety profile, encouraging further development. A systematic molecular modelling study was conducted to elucidate the mechanistic background of rosemary anti-aging properties through the inhibitory effects of its major constituents against key anti-aging targets viz. elastase, collagenase, and hyaluronidase. Development of rosemary extract lipid nanocapsules-based mucoadhesive gels was performed to improve skin contact, permeation, and bioavailability prior to in vivo testing. The developed formulae demonstrated small particle size (56.55-66.13 nm), homogenous distribution (PDI of 0.207-0.249), and negatively charged Zeta potential (- 13.4 to - 15.6). In UVB-irradiated rat model, topical rosemary hexane extract-loaded lipid nanocapsules-based gel provided photoprotection, restored the antioxidant biochemical state, improved epidermal and dermal histological features, and decreased the level of inflammatory and wrinkling markers. The use of rosemary hexane extract in anti-aging and photoprotective cosmeceuticals represents a safe, efficient, and cost-effective approach.


Assuntos
Nanocápsulas , Rosmarinus , Animais , Antioxidantes/farmacologia , Hexanos , Lipídeos , Compostos Fitoquímicos/farmacologia , Extratos Vegetais/química , Extratos Vegetais/farmacologia , Ratos , Rosmarinus/química
4.
Colloids Surf B Biointerfaces ; 211: 112299, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-34953364

RESUMO

The present study improved the effectiveness of a poorly water-soluble drug, luteolin (LUT), by encapsulating it in lecithin-bile salt-integrated system called bilosomes (BLs). Such a delivery system offers the benefits of mimicking the skin's biological structure and being a prominent tool to circumvent skin delivery obstacles. The prepared BLs underwent complete in vitro assessment. The developed BLs showed enhanced characteristics compared to free luteolin suspension (P < 0.05). Optimized BLs attained good entrapment efficiency (78.60% ± 0.88%), small particle size (226.1 ± 2.45 nm), and sustained drug-release pattern. The study also showed that both blank and LUT-loaded BLs preparations were safe to the skin with a primary irritancy index of < 2 based on the Draize test. In vivo tests were conducted to study the effect of the bile salt-based nanovesicles compared with the free LUT suspension. The photoprotective effect was evaluated according to the visual examination and biochemical analyses of antioxidant, anti-inflammatory, and anti-wrinkling markers after ultraviolet B irradiation. Results of biochemical markers and histopathological examination demonstrated that the LUT-BLs effect was superior than the LUT suspension (P < 0.05). Consequently, the current study proves that novel LUT-loaded BLs is a promising nanoplatform that overcome LUT delivery obstacles and, hence, alleviate UV-induced skin damage.


Assuntos
Lecitinas , Luteolina , Animais , Ácidos e Sais Biliares , Luteolina/farmacologia , Ratos , Ratos Wistar , Pele
5.
Pharm Dev Technol ; 26(6): 682-692, 2021 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-33952085

RESUMO

Although there are several treatments for rheumatoid arthritis (RA), outcomes are unsatisfactory and often associated with many side effects. We attempted to improve RA therapeutic outcomes by intra-articular administration of dual drug-loaded poly(lactic) acid (PLA)-coated herbal colloidal carriers (HCCs). Curcumin (CU) and resveratrol (RES) were loaded into HCCs because of their safety and significant anti-inflammatory activity. HCCs were prepared using a high-pressure, hot homogenization technique and evaluated in vitro and in vivo using a complete Freund's adjuvant-induced arthritis model. Transmission electron microscope (TEM) evaluated coating selected formulations with PLA, which increased particle sizes from 52 to 89.14 nm. The entrapment efficiency of both formulations was approximately 76%. HCCs significantly increased the amount of RES and CU released compared with the drug suspensions alone. The in vivo treated groups showed a significant improvement in joint healing. PLA-coated HCCs, followed by uncoated HCCs, yielded the highest reductions in knee diameter, myeloperoxidase (MPO) levels, and tumor necrosis factor-alpha (TNFα) levels. Histological examination of the dissected joints revealed that PLA-coated HCCs followed by uncoated HCCs exhibited the most significant joint healing effects. Our results demonstrate the superiority of intra-articularly administered HCCs to suppress RA progression compared with RES or CU suspensions alone.


Assuntos
Artrite Reumatoide/tratamento farmacológico , Coloides/administração & dosagem , Portadores de Fármacos/administração & dosagem , Preparações de Plantas/administração & dosagem , Poliésteres/administração & dosagem , Animais , Artrite Reumatoide/induzido quimicamente , Artrite Reumatoide/metabolismo , Coloides/metabolismo , Portadores de Fármacos/metabolismo , Adjuvante de Freund/toxicidade , Injeções Intra-Articulares/métodos , Masculino , Preparações de Plantas/metabolismo , Poliésteres/metabolismo , Ratos
6.
Drug Deliv Transl Res ; 8(3): 657-669, 2018 06.
Artigo em Inglês | MEDLINE | ID: mdl-29532355

RESUMO

Citalopram HCl (CH) is one of the few drugs which can be used safely in childhood psychiatric disorders. This study was focused on the preparation of interpenetrating polyelectrolytes nano-complexes (IPNC) to transform the hydrophilic carbohydrate polymers into an insoluble form. The IPNCs were loaded with CH to sustain its effect. The IPNC2 (composed of chitosan:pectin in a 3:1 ratio) showed the most extended drug release pattern (P < 0.05) and followed a Higuchi-order kinetics model. It was characterized using SEM, X-rays diffractometry, and FTIR. In-vivo studies were performed using immature rats with induced depression, and were based on the investigation of behavioral, biochemical, and histopathological changes at different time intervals up to 24 h. Rats treated with IPNC2 showed a significant more rapid onset of action and more extended effect in the behavioral tests, in addition to a significantly higher serotonin brain level up to 24 h, compared to rats treated with the market product (P < 0.05). The histopathological examination showed a profound amelioration of the cerebral cortex features of the depressed rats after IPNC2 administration. This study proves the higher efficacy and more extended effect of the new polyelectrolytes nano-complexes compared to the market product.


Assuntos
Antidepressivos de Segunda Geração/administração & dosagem , Quitosana/administração & dosagem , Citalopram/administração & dosagem , Nanoestruturas/administração & dosagem , Pectinas/administração & dosagem , Polieletrólitos/administração & dosagem , Inibidores Seletivos de Recaptação de Serotonina/administração & dosagem , Administração Oral , Animais , Antidepressivos de Segunda Geração/química , Comportamento Animal/efeitos dos fármacos , Encéfalo/efeitos dos fármacos , Encéfalo/patologia , Quitosana/química , Citalopram/química , Preparações de Ação Retardada/administração & dosagem , Preparações de Ação Retardada/química , Depressão/tratamento farmacológico , Depressão/patologia , Liberação Controlada de Fármacos , Masculino , Nanoestruturas/química , Pectinas/química , Polieletrólitos/química , Ratos , Inibidores Seletivos de Recaptação de Serotonina/química
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