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1.
Heliyon ; 10(7): e28457, 2024 Apr 15.
Artigo em Inglês | MEDLINE | ID: mdl-38586388

RESUMO

ß-carotene is obtained from both plants and animals and has been the subject of intense research because of its provitamin-A, antioxidant, and anticancer effects. Its limited absorption and oxidative degradation significantly reduce its antitumor efficacy when taken orally. In our study, we utilize a central composite design to develop "bio-safe and highly bio-compatible" solid lipid nanoparticles (SLNs) by using only the combination of palmitic acid and poloxamer-407, a block co-polymer as a surfactant. The current research aim to develop and characterize SLNs loaded with ß-carotene to improve their bioavailability and therapeutic efficacy. In addition, the improved cytotoxicity of solid lipid nanoparticles loaded with ß-carotene was screened in-vitro in human breast cancer cell lines (MCF-7). The nanoparticles exhibits good stability, as indicated by their mean zeta potential of -26.3 ± 1.3 mV. The particles demonstrated high drug loading and entrapment capabilities. The fabricated nanoparticle's prolonged release potential was shown by the in-vitro release kinetics, which showed a first-order release pattern that adhered to the Higuchi model and showed a slow, linear, and steady release over 48 h. Moreover, a diffusion-type release mechanism was used to liberate ß-carotene from the nanoparticles. For six months, the nanoparticles also showed a notable degree of physical stability. Lastly, using the MTT assay, the anti-cancer properties of ß-carotene-loaded solid lipid nanoparticles were compared with intact ß-carotene on MCF-7 cell lines. The cytotoxicity tests have shown that the encapsulation of ß-carotene in the lipid bilayers of the optimized formulation does not interfere with the anti-cancer activity of the drug. When compared to standard ß-carotene, ß-carotene loaded SLNs showed enhanced anticancer efficacy and it is a plausible therapeutic candidate for enhancing the solubility of water-insoluble and degradation-sensitive biotherapeutics like ß-carotene.

2.
J Vector Borne Dis ; 61(1): 107-116, 2024 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-38648412

RESUMO

BACKGROUND OBJECTIVES: Mosquitoes alone transmit diseases to around 700 million individuals annually, killing approximately 0.7 million people every year worldwide. Considering the potential health risks linked with synthetic repellents, it has become vital to identify eco-friendly, natural repellents for mosquito control as well as to understand the underlying mechanism for mosquito repellent activity. To address this, objectives were set to extract essential oils from Citrus macroptera peel and Homalomena aromatica (Spreng.) Schott. rhizomes, evaluate their mosquito repellent activity against Aedes aegypti, and further explore their mosquito odorant receptor inhibition potential. METHODS: The oils were extracted using Clevenger's apparatus, and properties like specific gravity, refractive index, and boiling point were evaluated and characterised using Fourier transform infrared spectroscopy (FTIR) and gas chromatography-mass spectroscopy (GC-MS). Aedes aegypti mosquito eggs collected from the Indian Council of Medical Research (ICMR), Dibrugarh, were reared in the Department of Pharmaceutical Sciences, Research Laboratory, to obtain adult Aedes aegypti mosquitoes for the mosquito repellent activity evaluation of the essential oils using the Human Bait technique'. Molecular docking studies were performed for the oil components against mosquito odorant binding proteins. Further, toxicity studies of these two oils were evaluated against human dermal fibroblast adult (HDFa) cells. RESULTS: The results revealed the presence of limonene (86.76%) and linalool (52.35%), respectively, in Citrus macroptera and Homalomena aromatica oils. It was found that the combination of the oils in a ratio of 1:1 showed mosquito repellent activity for up to 6.33 ± 0.23 h. Molecular docking studies showed the presence of major oil components having mosquito odorant receptor blocking potential comparable to N, N-diethyl-meta-toluamide (DEET), indicating a rationale for extended mosquito repellent action. Further, both of these oils were found to be non-cytotoxic against HDFa cells after 24 h. INTERPRETATION CONCLUSION: The encouraging mosquito repellent activity of these two oils as compared to synthetic mosquito repellent DEET might pave the way for the development of novel herbal mosquito repellent formulations containing these essential oils.


Assuntos
Aedes , Citrus , Repelentes de Insetos , Simulação de Acoplamento Molecular , Óleos Voláteis , Repelentes de Insetos/farmacologia , Repelentes de Insetos/química , Repelentes de Insetos/isolamento & purificação , Animais , Aedes/efeitos dos fármacos , Óleos Voláteis/farmacologia , Óleos Voláteis/química , Citrus/química , Humanos , Cromatografia Gasosa-Espectrometria de Massas , Espectroscopia de Infravermelho com Transformada de Fourier , Receptores Odorantes/metabolismo , Receptores Odorantes/química , Feminino , Rizoma/química
3.
ACS Omega ; 8(45): 43151-43162, 2023 Nov 14.
Artigo em Inglês | MEDLINE | ID: mdl-38024765

RESUMO

Myo-inositol hexakisphosphates (IHPs) or phytates are the most abundant organic phosphates having the potential to serve as a phosphorus reserve in soil. Understanding the fate of IHP interaction with soil minerals tends to be crucial for its efficient storage and utilization as a slow-release organic phosphate fertilizer. We have systematically compared the effective intercalation strategy of a phytate onto Zn-Fe layered double hydroxide (LDH) acting as storage/carrier material through coprecipitation and anion exchange. Powder X-ray diffraction, X-ray photoelectron spectroscopy, elemental analysis, thermogravimetric analysis, FTIR spectra, and molecular modeling demonstrated the formation of phytate-intercalated Zn-Fe LDH through coprecipitation with a maximum loading of 41.34% (w/w) in the pH range of ∼9-10 in a vertical alignment through monolayer formation. No intercalation product was obtained from the anion exchange method, which was concluded based on the absence of shifting in the XRD (003) peak. A change in the zeta potential values from positive to negative and subsequent increase in solution pH, with decreasing phytate concentration, are suggestive of adsorption of IHP onto the LDH surface. The batch adsorption data were best fitted with Langmuir isotherm equation and followed the pseudo-second-order kinetic model. The maximum adsorption capacity was found to be 45.87 mg g-1 at a temperature of 25 ± 0.5 °C and pH 5.63.

4.
Expert Opin Ther Pat ; 33(10): 681-699, 2023 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-37991186

RESUMO

INTRODUCTION: Nanotechnology may open up new avenues for overcoming the challenges of pancreatic cancer therapy as a broad arsenal of anticancer medicines fail to realize their full therapeutic potential in pancreatic ductal adenocarcinoma due to the formation of multiple resistance mechanisms inside the tumor. Many studies have reported the successful use of various nano formulations in pancreatic cancer therapy. AREAS COVERED: This review covers all the major nanotechnology-based patent litrature available on renowned patent data bases like Patentscope and Espacenet, through the time period of 2007-2022. This is an entirely patent centric review, and it includes both clinical and non-clinical data available on nanotechnology-based therapeutics and diagnostic tools for pancreatic cancer. EXPERT OPINION: For the sake of understanding, the patents are categorized under various formulation-specific heads like metallic/non-metallic nanoparticles, polymeric nanoparticles, liposomes, carbon nanotubes, protein nanoparticles and liposomes. This distinguishes one specific nanoparticle type from another and makes this review a one-of-a-kind comprehensive patent compilation that has not been reported so far in the history of nanotechnological formulations in pancreatic cancer.


Assuntos
Nanopartículas , Nanotubos de Carbono , Neoplasias Pancreáticas , Humanos , Lipossomos/uso terapêutico , Sistemas de Liberação de Medicamentos , Patentes como Assunto , Nanotecnologia , Neoplasias Pancreáticas/tratamento farmacológico
5.
Ther Deliv ; 14(9): 543-569, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-37671556

RESUMO

Atopic dermatitis is a prevalent chronic skin inflammation affecting 2.1 to 4.1% of adults globally. The complexity of its pathogenesis and the relapsing nature make it challenging to treat. Current treatments follow European Academy of Dermatology and Venerology guidelines, but advanced cases with recurring lesions lack effective therapies. To address this gap, researchers are exploring nanotechnology for targeted drug delivery. Nanoparticles offer benefits such as improved drug retention, stability, controlled release and targeted delivery through the disrupted epidermal barrier. This integrated review evaluates the current state of AD treatment and highlights the potential of novel nano-formulations as a promising approach to address the disease.


Atopic dermatitis is a skin disease and difficult to treat. It happens because of various reasons like skin barrier problems, weather conditions, irritants and allergens from microorganisms. The current treatments do not fully cure the disease, and there's no established treatment for it but there is hope in nanotechnology and nanoformulations. Nano formulations are preparations with particles between 8 and 250 nm. Moreover, studies with animals and humans show promising results with nanoformulations. This review paper explores different ways to use nanotechnology to treat atopic dermatitis. It might lead to exciting new treatments in the future.


Assuntos
Dermatite Atópica , Adulto , Humanos , Dermatite Atópica/tratamento farmacológico , Dermatite Atópica/etiologia , Dermatite Atópica/patologia , Inflamação/tratamento farmacológico , Epiderme , Sistemas de Liberação de Medicamentos , Nanotecnologia
6.
Curr Cancer Drug Targets ; 23(8): 620-633, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-36843367

RESUMO

Pancreatic ductal adenocarcinoma (PDAC) is one of the foremost causes of cancer-related morbidities worldwide. Novel nanotechnology-backed drug delivery stratagems, including molecular targeting of the chemotherapeutic payload, have been considered. However, no quantum leap in the gross survival rate of patients with PDAC has been realized. One of the predominant causes behind this is tumor desmoplasia, a dense and heterogenous stromal extracellular matrix of the tumor, aptly termed tumor microenvironment (TME). It plays a pivotal role in the tumor pathogenesis of PDAC as it occupies most of the tumor mass, making PDAC one of the most stromal-rich cancers. The complex crosstalk between the tumor and dynamic components of the TME impacts tumor progression and poses a potential barrier to drug delivery. Understanding and deciphering the complex cascade of tumorstromal interactions are the need of the hour so that we can develop neoteric nano-carriers to disrupt the stroma and target the tumor. Nanodiamonds (NDs), due to their unique surface characteristics, have emerged as a promising nano delivery system in various pre-clinical cancer models and have the potential to deliver the chemotherapeutic payload by moving beyond the dynamic tumor-stromal barrier. It can be the next revolution in nanoparticle-mediated pancreatic cancer targeting.


Assuntos
Carcinoma Ductal Pancreático , Nanodiamantes , Neoplasias Pancreáticas , Humanos , Nanodiamantes/uso terapêutico , Terapia de Alvo Molecular , Neoplasias Pancreáticas/tratamento farmacológico , Neoplasias Pancreáticas/patologia , Carcinoma Ductal Pancreático/tratamento farmacológico , Carcinoma Ductal Pancreático/patologia , Microambiente Tumoral , Neoplasias Pancreáticas
7.
Pharm Nanotechnol ; 10(4): 268-278, 2022 11 15.
Artigo em Inglês | MEDLINE | ID: mdl-35946098

RESUMO

The eye is a one-of-a-kind sensory organ with intricate anatomy and physiology. It is protected by a variety of barriers, ranging from static barriers to dynamic barriers. Although these barriers are very effective at protecting the eye from exogenous substances and external stress, they are highly compromised by various vision-impairing diseases of both the anterior and the posterior segment of the eye. Due to ocular elimination systems and intricate obstacles that selectively limit drug entry into the eye, effective drug delivery to the posterior segment of the eye (PSE) continues to be a challenge in ophthalmology. Since more than half of the most debilitating eye illnesses are thought to originate in the posterior segment (PS), understanding the physiology and clearance mechanism of the eye could help design improved formulations that could be noninvasive and intended for targeted posterior segment therapeutics. Moreover, the major drawback associated with the conventional drug delivery system to PSE is minimal therapeutic drug concentration in the desired ocular tissue and life-threatening ophthalmic complications. One possible approach that can be implemented to overcome these ocular barriers for efficient ocular therapy, non-invasive and targeted drug action to the posterior tissues is by designing nanomedicines. This review summarizes the recent non-invasive and patient compliant advances in designing nanomedicines targeting PSE. The various routes and pathways of drug administration to the ocular tissue are also summarized.


Assuntos
Oftalmopatias , Humanos , Oftalmopatias/tratamento farmacológico , Oftalmopatias/metabolismo , Olho/metabolismo , Sistemas de Liberação de Medicamentos , Nanomedicina , Preparações Farmacêuticas
9.
J Vasc Nurs ; 40(1): 2-10, 2022 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-35287830

RESUMO

BACKGROUND: For Melatonin, the pineal gland hormone, also known as the neuroendocrine hormone, influences angiogenesis by exerting a positive effect on fibroblast, monocyte, and cytokine proliferation. Formulation and study of characteristics of gelation-based Melatonin sponge crosslinked with fructose using the surfactant foaming and freeze-drying method for wound healing application was the objective of our study. The structure of the formulated gelatin sponge was observed using a scanning electron microscope and showed to have abundant and uniform pores. Characteristics were studied using digestibility test, water uptake test, porosity measurement test, moisture uptake test, tensile strength test, folding endurance test, scanning electron microscopy, Fourier transform infrared spectroscopy, and drug entrapment efficiency analysis. RESULTS: The obtained data showed that the formulated sponge had good mechanical properties, water uptake, and water retention capacities. In animal experiments, histological and macroscopic observations showed that wounds covered by gelatin loaded with a Melatonin sponge healed quickly. CONCLUSION: The formulated sponge was a potential wound healing material having suitable physical, mechanical properties and biocompatibility. The graphical abstract is shown in Figure 1.


Assuntos
Gelatina , Melatonina , Animais , Bandagens , Materiais Biocompatíveis/química , Gelatina/química , Humanos , Melatonina/farmacologia , Água
10.
Pharm Nanotechnol ; 10(1): 42-55, 2022.
Artigo em Inglês | MEDLINE | ID: mdl-34951376

RESUMO

BACKGROUND: The brain is a vital and composite organ. By nature, the innate make-up of the brain is such that in anatomical parlance, it is highly protected by the "Blood-Brain Barrier", which is a nexus of capillary endothelial cells, basement membrane, neuroglial membrane and glialpodocytes. The same barrier, which protects and isolates the interstitial fluid of the brain from capillary circulation, also restricts the therapeutic intervention. Many standing pharmaceutical formulations are ineffective in the treatment of inimical brain ailments because of the inability of the API to surpass and subsist inside the Blood Brain Barrier. OBJECTIVE: This is an integrated review that emphasizes on the recent advancements in brain-targeted drug delivery utilizing nanodiamonds (NDs) as a carrier of therapeutic agents. NDs are a novel nanoparticulate drug delivery system, having carbon moieties as their building blocks and their surface tenability is remarkable. These neoteric carbon-based carriers have exceptional, mechanical, electrical, chemical, optical, and biological properties, which can be further rationally modified and augmented. DISCUSSION: NDs could be the next"revolution "in the field of nanoscience for the treatment of neurodegenerative disorders, brain tumors, and other pernicious brain ailments. What sets them apart from other nanocarriers is their versatile properties like diverse size range and surface modification potential, which makes them efficient enough to move across certain biological barriers and offer a plethora of brain targeting and bioimaging abilities. CONCLUSION: The blood-brain barrier (BBB) poses a major hurdle in the way of treating many serious brain ailments. A range of nanoparticle based drug delivering systems have been formulated, including solid lipid nanoparticles, liposomes, dendrimers, nanogels, polymeric NPs, metallic NPs (gold, platinum, andironoxide) and diamondoids (carbonnanotubes). Despite this development, only a few of these formulations have shown the ability to cross the BBB. Nanodiamonds, because of their small size, shape, and surface characteristics, have a potential in moving beyond the diverse and intricate BBB, and offer a plethora of brain targeting capabilities.


Assuntos
Nanodiamantes , Encéfalo/diagnóstico por imagem , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Células Endoteliais , Humanos , Lipossomos , Nanopartículas
11.
Drug Dev Ind Pharm ; 47(8): 1326-1334, 2021 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-34633264

RESUMO

OBJECTIVE: Development of Frostbite healing hydrogel of Manuka honey and hyaluronic acid. SIGNIFICANCE: Frostbite is a cold-induced ischemic vascular injury non-responsive to most of the wound healing products. Thrombus-induced ischemia is the main cause of frostbite-related necrosis. Hyaluronic acid is known to possess significant antithrombotic and wound healing activity. Moreover, Manuka Honey is also rich in flavonoids and polyphenols with potential antithrombotic activity. These two agents were together utilized to develop a frostbite healing formulation. METHODS: In-silico antithrombotic efficacy of major phytoconstituents of Manuka honey was evaluated using in-silico-docking studies against Tissue plasminogen activator and Cyclooxygenase-1 protein. Further in-vivo frostbite healing evaluation was carried out in Wistar rats, by inducing frostbite with a supercooled rod. RESULTS: The results indicate that major leptosin and other major phytoconstituent of Manuka honey has significant antithrombotic property. The hydrogel formulation of HA and MH possess significant antimicrobial efficacy. The wound contraction studies and histopathological evaluation reveals that the hydrogel also has a good frostbite healing activity showing complete wound healing within an 18-day period. The findings of the western blotting studies suggest that the hydrogel acts by VEGF- NRF-2 pathway. CONCLUSION: This result implies that the prepared hydrogel can serve as an effective frostbite healing formulation.


Assuntos
Congelamento das Extremidades , Mel , Animais , Fibrinolíticos/farmacologia , Congelamento das Extremidades/tratamento farmacológico , Ácido Hialurônico/farmacologia , Hidrogéis , Ratos , Ratos Wistar , Ativador de Plasminogênio Tecidual/farmacologia , Cicatrização
12.
J Biomater Sci Polym Ed ; 32(11): 1420-1449, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-33941041

RESUMO

Mucoadhesive microspheres have their own significant amongst the various sustained release drug delivery systems. The prolonged residence time of these delivery devices at drug absorption site results in steep concentration gradient and enhanced bioavailability. In this study, the mucilage of Isabgol husk was applied as polymeric backbone to develop gliclazide loaded microspheres by crosslinking with glutaraldehyde. The formulations were studied for surface morphology, swelling behavior, particle size, in vitro release, release kinetics, in vitro mucoadhesion and gamma scintigraphy in rabbits. The release of gliclazide from microspheres was controlled by swelling of crosslinked microspheres followed by diffusion. Gamma scintigraphic images acquired for microspheres retention in gastrointestinal track of rabbits indicated the residence of formulation upto 24 h after oral administration. Gliclazide retained its integrity in polymeric matrix of microspheres as observed by Fourier transform infrared spectroscopy, differential scanning calorimetry and powder X-ray diffractometry. The sustained release of gliclazide and prolonged retention of microspheres in gastrointestinal track disclosed the rationality of mucoadhesive Isabgol husk microspheres in controlling the hyperglycemia in diabetes.


Assuntos
Gliclazida , Animais , Preparações de Ação Retardada , Sistemas de Liberação de Medicamentos , Glutaral , Microesferas , Tamanho da Partícula , Coelhos
13.
Sci Rep ; 11(1): 3357, 2021 02 08.
Artigo em Inglês | MEDLINE | ID: mdl-33558597

RESUMO

Burn injuries are most challenging to manage since it causes loss of the integrity of large portions of the skin leading to major disability or even death. Over the years, hydrogels are considered as a significant delivery system for wound treatment because of several advantages over other conventional formulations. We hypothesized that the bFGF-collagen-AgSD incorporated hydrogel formulation can accelerate the rate of burn healing in animal model and would promote fibroblast cell proliferation. Neovascularization and re-epithelialization is a hall mark of burn wound healing. In the present study, histopathological investigation and scanning electron microscopy of skin tissue of Wistar rats showed almost complete epithelialisation after 16 days in the treatment group. The developed hydrogel showed significantly accelerated wound closure compared with a standard and control group. The faster wound closure resulted from increased re-epithelialization and granulation tissue formation because of the presence of collagen and growth factor. Expressions of proteins such as TrkA, p- TrkA, ERK1/2, p-ERK1/2, NF-kß, and p-NF-kß involved in nerve growth factor (NGF) signalling pathway were analysed by western blot. All the findings obtained from this study indicated that the hydrogel can be considered as a promising delivery system against second degree burn by faster healing.


Assuntos
Queimaduras , Colágeno/farmacologia , Fator 2 de Crescimento de Fibroblastos/farmacologia , Hidrogéis/farmacologia , Sistema de Sinalização das MAP Quinases/efeitos dos fármacos , Animais , Queimaduras/tratamento farmacológico , Queimaduras/metabolismo , Queimaduras/patologia , Colágeno/química , Fator 2 de Crescimento de Fibroblastos/química , Hidrogéis/química , Inflamação/tratamento farmacológico , Inflamação/metabolismo , Inflamação/patologia , Proteína Quinase 1 Ativada por Mitógeno/metabolismo , Proteína Quinase 3 Ativada por Mitógeno/metabolismo , Ratos , Ratos Wistar , Receptor trkA/metabolismo
14.
J Therm Biol ; 93: 102716, 2020 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-33077129

RESUMO

Frostbite is a severe ischemic injury which occurs due to the tissue vascular damage after sub-zero temperature tissue exposure. Deep frostbite can result in necrosis and may need amputation of affected tissue. Though a serious injury, it is not very well understood, and further scientific exploration is needed. This work explores the current understanding of the pathophysiology of frostbite. We reviewed the current status of the diagnostics, the drugs, the therapies and the surgical practices for prevention and management of frostbite. Advances in nanotechnology and drug delivery had improved the therapeutic outcomes significantly. This review also explored the latest advancements and researches done for development of newer therapeutics and diagnostics for frostbite care.


Assuntos
Congelamento das Extremidades/terapia , Amputação Cirúrgica/métodos , Animais , Congelamento das Extremidades/diagnóstico , Congelamento das Extremidades/etiologia , Humanos , Oxigenoterapia Hiperbárica/métodos , Guias de Prática Clínica como Assunto , Terapia Trombolítica/métodos
15.
J Food Sci Technol ; 57(4): 1205-1215, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32180617

RESUMO

Grapes are one of the most highly consumed fruits across the world. In ancient Europe the leaves and the sap of grape plants has been used in traditional treatment for ages. Besides being a wellspring for vitamins and fibre, the skin and seeds of grapes are highly rich in Polyphenols specifically proanthocyanidins, which can be used as a functional ingredient to address various health issues by boosting the natural bio-processes of the body. Since, grape seeds are by product of wine making companies therefore can be easily procured. The present review article briefly describes the various pharmacological activities of grape seed extract and different experimental studies were done which supports the beneficial health qualities of the extract. Through different and various studies, it was proved that the proanthocyanidin rich grape seed extract provides benefits against many diseases i.e. inflammation, cardiovascular disease, hypertension, diabetes, cancer, peptic ulcer, microbial infections, etc. Therefore, beside from using it as a nutraceutical or cosmeceutical, as a result they may have a potential to substitute or complement in currently used drugs in the treatment of diseases by developing it into other successful pharmaceutical formulations for better future prospective.

16.
Carbohydr Polym ; 230: 115664, 2020 Feb 15.
Artigo em Inglês | MEDLINE | ID: mdl-31887927

RESUMO

Erlotinib-loaded carboxymethyl temarind gum-g-poly(N-isopropylacrylamide)-montmorillonite based semi-IPN nanocomposites were synthesized and characterized for their in vitro performances for lung cancer therapy. The placebo matrices exhibited outstanding biodegradability and pH-dependent swelling profiles. The molar mass (M¯ c) between the crosslinks of these composites was declined with temperature. The solid state characterization confirmed the semi-IPN architecture of these scaffolds. The corresponding drug-loaded formulations displayed excellent drug-trapping capacity (DEE, 86-97 %) with acceptable zeta potential (-16 to -13 mV) and diameter (967-646 nm). These formulations conferred sustained drug elution profiles (Q8h, 77-99 %) with an initial burst release. The drug release profile of the optimized formulation (F-3) was best fitted in the first order kinetic model with Fickian diffusion driven mechanism. The mucin adsorption to F-3 followed Langmuir isotherms. The results of MTT assay, AO/EB staining and confocal analyses revealed that the ERL-loaded formulation suppressed A549 cell proliferation and induced apoptosis more effectively than pristine drug.


Assuntos
Portadores de Fármacos/química , Cloridrato de Erlotinib/administração & dosagem , Nanocompostos/química , Células A549 , Portadores de Fármacos/uso terapêutico , Liberação Controlada de Fármacos , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Nanocompostos/uso terapêutico
17.
Drug Dev Ind Pharm ; 45(8): 1332-1341, 2019 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-31116617

RESUMO

The present study is aimed at the development of a sunscreen cream for use in high altitude areas which have been found to possess superior sun protection factor (SPF) along with remarkable antioxidant activity. The topical formulation is a standard oil-in-water emulsion of a combination of United States Food and Drug Administration (US FDA) approved ultraviolet filters; along with melatonin and pumpkin seed oil. The in-silico optimized formulation was characterized using established methods and the stability study was carried out as per International Conference on Harmonization guidelines. The formulation was prepared after requisite pre-formulation analysis by Fourier-transform infrared spectroscopy, differential scanning calorimetric and thermogravimetric analyses; followed by characterization based on color, odor, phase separation, spreadability, specific gravity, homogeneicity, centrifugation and sensitivity. For the stability study, a total of three samples from three batches of the finished product were subjected to the stability study. The samples were analyzed for content uniformity, pH, in vitro SPF, rheology, zeta potential, droplet diameter and microbial analysis of the 0th day and also the the end of the storage period. Results obtained from the stability study indicated that the formulation possesses 50+ in vitro SPF value and remained stable for 6 months and 12 months under storage at 40 ± 2 °C and 75 ± 5% relative humidity; and -20 °C ± 5 °C respectively.


Assuntos
Protetores Solares/química , Altitude , Química Farmacêutica/métodos , Pele/efeitos dos fármacos , Fator de Proteção Solar/métodos , Raios Ultravioleta/efeitos adversos
18.
Immunopharmacol Immunotoxicol ; 41(1): 130-139, 2019 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-30741582

RESUMO

Objective: Melatonin and pumpkin seed oil, along with US FDA approved UV filters were incorporated into a formulation for enhancement of UV protection by exerting an antioxidant effect. The objective of this study was to assess the protective effect of this formulation against ultraviolet (UV) radiation-induced photo dermatitis in rats, which is an established model to study the aetiopathogenic mechanisms in psoriasis vulgaris, as the former exhibits the same features to those of clinical psoriasis vulgaris in humans. Materials and methods: The animals were segregated into five groups (6/group) and all received their respective formulations dermally prior to chronic UV irradiation for 28 days. The test, placebo, and standard groups; received the test, placebo, and standard formulations respectively; whereas the positive control group received only UV radiation. A normal control group was also maintained. Disease and treatment status were analyzed using various techniques by euthanizing the rats after 28 days. Results: The test formulation was able to ameliorate the UV-induced increase in skin fold, epidermal thickness, and skin edema; inhibit the reduction of hydroxyproline content and incidence of LPO within the skin tissues of exposed animals. The formulation was also able to inhibit the release of proinflammatory cytokines; IFN-γ, IL-1ß, IL-6, and TNF-α; and upregulation of NF-κB and COX-2 genes caused by chronic UV exposure. Conclusion: It can be stated that melatonin included in the newly formulated sunscreen was able to inhibit the induction of photodermatitis via immunoregulation of inflammatory cytokines along with NF-κB and COX-2 genes.


Assuntos
Melatonina/farmacologia , NF-kappa B/antagonistas & inibidores , Transtornos de Fotossensibilidade/prevenção & controle , Pele/efeitos dos fármacos , Protetores Solares/farmacologia , Raios Ultravioleta , Animais , Antioxidantes/metabolismo , Modelos Animais de Doenças , Relação Dose-Resposta a Droga , Combinação de Medicamentos , Masculino , Melatonina/administração & dosagem , NF-kappa B/genética , Transtornos de Fotossensibilidade/imunologia , Transtornos de Fotossensibilidade/patologia , Psoríase/etiologia , Psoríase/imunologia , Psoríase/prevenção & controle , Ratos Wistar , Pele/imunologia , Pele/patologia , Protetores Solares/administração & dosagem
19.
Eur J Ophthalmol ; 29(1): 113-126, 2019 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-29756507

RESUMO

Delivery of drugs to eyes is a great challenge to researchers because of a number of barriers in the eye preventing the actual dose from reaching the site. A number of ophthalmic delivery systems have been developed in the past couple of years that are not only new but also safe and reliable and help to overcome all those barriers in the eye which are responsible for the very less bioavailability of drugs. In this review, we tried to focus on current research in ocular delivery of drug substances giving special emphasis to liposomal delivery system. A brief analysis of other novel ocular delivery systems, ocular physiology, and microbial sources of disease are also highlighted herein. We analyzed the various research findings for churning a general idea for novel ocular delivery system and its future use. The novel formulations may overcome the addressed problems of ophthalmic medication and comply with the quality assurance issues. The liposomal delivery is advantageous as they have the ability to entrap both hydrophobic and hydrophilic drugs and are suitable for delivery to both the anterior and posterior segment of the eye. Therefore, the use of this alternative approach is quite a necessity.


Assuntos
Sistemas de Liberação de Medicamentos , Oftalmopatias/tratamento farmacológico , Lipossomos , Preparações Farmacêuticas/administração & dosagem , Administração Oftálmica , Animais , Humanos , Interações Hidrofóbicas e Hidrofílicas , Soluções Oftálmicas/uso terapêutico
20.
Curr Drug Deliv ; 16(1): 26-41, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-30227817

RESUMO

Wound infections impose a remarkable clinical challenge that has a considerable influence on morbidity and mortality of patients, influencing the cost of treatment. The unprecedented advancements in molecular biology have come up with new molecular and cellular targets that can be successfully applied to develop smarter therapeutics against diversified categories of wounds such as acute and chronic wounds. However, nanotechnology-based diagnostics and treatments have achieved a new horizon in the arena of wound care due to its ability to deliver a plethora of therapeutics into the target site, and to target the complexity of the normal wound-healing process, cell type specificity, and plethora of regulating molecules as well as pathophysiology of chronic wounds. The emerging concepts of nanobiomaterials such as nanoparticles, nanoemulsion, nanofibrous scaffolds, graphene-based nanocomposites, etc., and nano-sized biomaterials like peptides/proteins, DNA/RNA, oligosaccharides have a vast application in the arena of wound care. Multi-functional, unique nano-wound care formulations have acquired major attention by facilitating the wound healing process. In this review, emphasis has been given to different types of nanomaterials used in external wound healing (chronic cutaneous wound healing); the concepts of basic mechanisms of wound healing process and the promising strategies that can help in the field of wound management.


Assuntos
Fármacos Dermatológicos/administração & dosagem , Portadores de Fármacos/química , Nanoestruturas/química , Cicatrização/efeitos dos fármacos , Infecção dos Ferimentos/terapia , Administração Cutânea , Doença Crônica/epidemiologia , Doença Crônica/terapia , Humanos , Morbidade , Pele/efeitos dos fármacos , Pele/lesões , Resultado do Tratamento , Infecção dos Ferimentos/epidemiologia
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