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1.
Microb Pathog ; 186: 106494, 2024 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-38065294

RESUMO

Bacterial vaginosis (BV) is a recurring, chronic infection that is difficult to treat due to the limited bioavailability of antimicrobials within vaginal epithelial cells. Vaginal administration, because of lower dosing and systemic exposure offers a viable option for treating vaginal infections. In this study, Metronidazole-loaded chitosan nanoparticles were synthesised employing borax (BX) or tannic acid (TA) as an antimicrobial crosslinking agent for treating BV. The prepared NPs were characterized for various physical, physicochemical, pharmaceutical, thermal and antibacterial properties. Morphological investigation revealed that nanoparticles prepared from 0.5 % w/v chitosan, 1.2 % w/v BX, and 0.4 % w/v metronidazole (MTZ) were non-spherical, with particle sizes of 377.4 ± 37.3 nm and a zeta potential of 34 ± 2.1 mV. The optimised formulation has MIC values of 24 ± 0.5 and 59 ± 0.5 µg/mL, against Escherichia coli (E.coli) and Candida albicans (C.albicans) respectively. The results of DSC and XRD demonstrated no change in the physical state of the drug in the finished formulation. Under simulated vaginal fluid, the optimised formulation demonstrates a cumulative drug release of about 90 % within 6h. The prepared borax crosslinked NPs exhibit anti-fungal activities by inhibiting ergosterol synthesis. The in-vivo antibacterial data indicated a comparable reduction in bacterial count compared to the marketed formulation in female Swiss albino mice treated with optimised nanoparticles. According to histopathological findings, the prepared nanoparticle was safe for vaginal use. Based on the experimental findings, it was concluded that MBCSNPs, due to their good physiochemical and antimicrobial properties, could serve as a potential topical alternative for treating BV and reducing fungal infection.


Assuntos
Quitosana , Nanopartículas , Vaginose Bacteriana , Feminino , Humanos , Animais , Camundongos , Metronidazol/farmacologia , Vaginose Bacteriana/tratamento farmacológico , Quitosana/química , Portadores de Fármacos/química , Antibacterianos/química , Nanopartículas/química , Tamanho da Partícula
2.
AAPS PharmSciTech ; 25(3): 57, 2024 Mar 12.
Artigo em Inglês | MEDLINE | ID: mdl-38472545

RESUMO

Psoriasis is a complex and persistent autoimmune skin disease. The present research focused on the therapeutic evaluation of betulin-loaded nanostructured lipid carriers (BE-NLCs) towards managing psoriasis. The BE-NLCs were synthesized using the emulsification cum solidification method, exhibiting a spherical shape with a particle size of 183.5±1.82nm and a narrow size distribution window (PDI: 0.142±0.05). A high zeta potential -38.64±0.05mV signifies the relative stability of the nano-dispersion system. BE-NLCs show a drug loading and entrapment efficiency of 47.35±3.25% and 87.8±7.86%, respectively. In vitro release study, BE NLCs show a cumulative percentage release of 90.667±5.507% over BE-sol (57.334±5.03%) and BD-oint (42±4.58%) for 720min. In an ex vivo 24-h permeation study, % cumulative amount permeated per cm2 was found to be 55.667±3.33% from BE-NLCs and 32.012±3.26% from BE-sol, demonstrating a better permeability of 21.66% when compared to the standard formulation BD-oint. The in vivo anti-psoriatic activity in the IMQ-induced model shows topical application of BE-sol, BE-NLCs, and BD-oint resulted in recovery rates of 56%, 82%, and 65%, respectively, based on PASI (Psoriasis Area and Severity Index) score. Notably, BE-NLCs demonstrated a more significant reduction in spleen mass, indicating attenuation of the local innate immune system in psoriatic mice. Reductions in TNF-α, IL-6, and IL-17 levels were observed in both BE-sol and BE-NLCs groups compared to the disease control (DC) group, with BE-NLCs exhibiting superior outcomes (74.05%, 44.76%, and 49.26% reduction, respectively). Soy lecithin and squalene-based NLCs could be better carrier system for the improvement of the therapeutic potential of BE towards management of psoriasis.


Assuntos
Ácido Betulínico , Nanoestruturas , Psoríase , Camundongos , Animais , Imiquimode/efeitos adversos , Portadores de Fármacos/uso terapêutico , Psoríase/tratamento farmacológico , Lipídeos , Tamanho da Partícula
3.
AAPS PharmSciTech ; 25(4): 85, 2024 Apr 11.
Artigo em Inglês | MEDLINE | ID: mdl-38605158

RESUMO

Cervical cancer (CC) is the fourth leading cancer type in females globally. Being an ailment of the birth canal, primitive treatment strategies, including surgery, radiation, or laser therapy, bring along the risk of infertility, neonate mortality, premature parturition, etc. Systemic chemotherapy led to systemic toxicity. Therefore, delivering a smaller cargo of therapeutics to the local site is more beneficial in terms of efficacy as well as safety. Due to the regeneration of cervicovaginal mucus, conventional dosage forms come with the limitations of leaking, the requirement of repeated administration, and compromised vaginal retention. Therefore, these days novel strategies are being investigated with the ability to combat the limitations of conventional formulations. Novel carriers can be engineered to manipulate bioadhesive properties and sustained release patterns can be obtained thus leading to the maintenance of actives at therapeutic level locally for a longer period. Other than the purpose of CC treatment, these delivery systems also have been designed as postoperative care where a certain dose of antitumor agent will be maintained in the cervix postsurgical removal of the tumor. Herein, the most explored localized delivery systems for the treatment of CC, namely, nanofibers, nanoparticles, in situ gel, liposome, and hydrogel, have been discussed in detail. These carriers have exceptional properties that have been further modified with the aid of a wide range of polymers in order to serve the required purpose of therapeutic effect, safety, and stability. Further, the safety of these delivery systems toward vital organs has also been discussed.


Assuntos
Antineoplásicos , Nanopartículas , Neoplasias do Colo do Útero , Feminino , Recém-Nascido , Humanos , Neoplasias do Colo do Útero/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Lipossomos , Hidrogéis
4.
AAPS PharmSciTech ; 25(5): 106, 2024 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-38724834

RESUMO

The primary factor underlying the virulence of Candida albicans is its capacity to form biofilms, which in turn leads to recurrent complications. Over-the-counter antifungal treatments have proven ineffective in eliminating fungal biofilms and the inflammatory cytokines produced during fungal infections. Chitosan nanoparticles offer broad and versatile therapeutic potential as both antifungal agents and carriers for antifungal drugs to combat biofilm-associated Candida infections. In our study, we endeavoured to develop chitosan nanoparticles utilising chitosan and the antifungal crosslinker phytic acid targeting C. albicans. Phytic acid, known for its potent antifungal and anti-inflammatory properties, efficiently crosslinks with chitosan. The nanoparticles were synthesised using the ionic gelation technique and subjected to analyses including Fourier transform infrared spectroscopy, dynamic light scattering, and zeta potential analysis. The synthesised nanoparticles exhibited dimensions with a diameter (Dh) of 103 ± 3.9 nm, polydispersity index (PDI) of 0.33, and zeta potential (ZP) of 37 ± 2.5 mV. These nanoparticles demonstrated an antifungal effect with a minimum inhibitory concentration (MIC) of 140 ± 2.2 µg/mL, maintaining cell viability at approximately 90% of the MIC value and reducing cytokine levels. Additionally, the nanoparticles reduced ergosterol content and exhibited a 62% ± 1.2 reduction in biofilm susceptibility, as supported by colony-forming unit (CFU) and XTT assays-furthermore, treatment with nanoparticles reduced exopolysaccharide production and decreased secretion of aspartyl protease by C. albicans. Our findings suggest that the synthesised nanoparticles effectively combat Candida albicans infections. In vivo studies conducted on a mouse model of vaginal candidiasis confirmed the efficacy of the nanoparticles in combating fungal infections in vivo.


Assuntos
Anti-Inflamatórios não Esteroides , Antifúngicos , Biofilmes , Candida albicans , Candidíase Vulvovaginal , Quitosana , Reagentes de Ligações Cruzadas , Nanopartículas , Ácido Fítico , Biofilmes/efeitos dos fármacos , Ácido Fítico/química , Ácido Fítico/farmacologia , Ácido Fítico/uso terapêutico , Reagentes de Ligações Cruzadas/química , Reagentes de Ligações Cruzadas/farmacologia , Reagentes de Ligações Cruzadas/uso terapêutico , Quitosana/química , Quitosana/farmacologia , Quitosana/uso terapêutico , Nanopartículas/química , Nanopartículas/uso terapêutico , Antifúngicos/química , Antifúngicos/farmacologia , Antifúngicos/uso terapêutico , Anti-Inflamatórios não Esteroides/química , Anti-Inflamatórios não Esteroides/farmacologia , Anti-Inflamatórios não Esteroides/uso terapêutico , Testes de Sensibilidade Microbiana , Citocinas/imunologia , Candida albicans/efeitos dos fármacos , Candida albicans/patogenicidade , Feminino , Animais , Camundongos , Candidíase Vulvovaginal/tratamento farmacológico , Candidíase Vulvovaginal/metabolismo , Vagina/microbiologia
5.
AAPS PharmSciTech ; 25(2): 31, 2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38326518

RESUMO

Drug delivery to the buccal mucosa is one of the most convenient ways to treat common mouth problems. Here, we propose a spray-dried re-dispersible mucoadhesive controlled release gargle formulation to improve the efficacy of chlorhexidine. The present investigation portrays an approach to get stable and free-flowing spray-dried porous aggregates of chlorhexidine-loaded sodium alginate nanoparticles. The ionic gelation technique aided with the chlorhexidine's positive surface charge-based crosslinking, followed by spray drying of the nanoparticle's dispersion in the presence of lactose- and leucine-yielded nano-aggregates with good flow properties and with a size range of about 120-350 nm. Provided with the high entrapment efficiency (87%), the particles showed sustained drug release behaviors over a duration of 10 h, where 87% of the released drug got permeated within 12 h. The antimicrobial activity of the prepared formulation was tested on S. aureus, provided with a higher zone of growth inhibition than the marketed formulation. Aided with an appropriate mucoadhesive strength, this product exhibited extended retention of nanoparticles in the throat region, as shown by in vivo imaging results. In conclusion, the technology, provided with high drug retention and extended effect, could be a potential candidate for treating several types of throat infections.


Assuntos
Clorexidina , Faringe , Staphylococcus aureus , Sistemas de Liberação de Medicamentos/métodos , Preparações de Ação Retardada , Antissépticos Bucais , Tamanho da Partícula
6.
Pharm Dev Technol ; 28(1): 78-94, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36564887

RESUMO

Oral mucositis is a serious issue in patients receiving oncological therapies. Mucosal protectants considered to be one of the preferred choices used in the management of mucositis. However, the protective efficacy of currently available mucosal protectants has been significantly compromised due to poor retention, lack of lubrication, poor biodegradability, and inability to manage secondary complications. Chitosan is a promising material for mucosal applications due to its beneficial biomedical properties. Chitosan is also anti-inflammatory, anti-microbial, and capable of scavenging free radicals, makes it a good candidate for the treatment of oral mucositis. Additionally, chitosan's amino polysaccharide skeleton permits a number of chemical alterations with better bioactive performance. This article provides a summary of key biological properties of chitosan and its derivatives that are useful for treating oral mucositis. Current literature evidence shows that Chitosan has superior mucosal protective properties when utilised alone or as delivery systems for co-encapsulated drugs.


Assuntos
Quitosana , Neoplasias , Estomatite , Humanos , Quitosana/química , Materiais Biocompatíveis , Estomatite/tratamento farmacológico , Estomatite/etiologia , Neoplasias/tratamento farmacológico
7.
AAPS PharmSciTech ; 24(7): 196, 2023 Oct 02.
Artigo em Inglês | MEDLINE | ID: mdl-37783948

RESUMO

Despite having a wide range of therapeutic advantages, glycyrrhizin (GL) has few commercial applications due to its poor aqueous solubility. In this study, we combined the benefits of hydroxypropyl ß-cyclodextrin (HP-ßCD) supramolecular inclusion complexes and electrospun nanofibers to improve the solubility and therapeutic potential of GL. A molecular inclusion complex containing GL and HP-ßCD was prepared by lyophilization at a 1:2 molar ratio. GL and hydroxypropyl ß-cyclodextrin inclusion complexes were also incorporated into hyaluronic acid (HA) nanofibers. Prepared NF was analyzed for physical, chemical, thermal, and pharmaceutical properties. Additionally, a rat model of carrageenan-induced hind paw edema and macrophage cell lines was used to evaluate the anti-inflammatory activity of GL-HP-ßCD NF. The DSC and XRD analyses clearly showed the amorphous state of GL in nanofibers. In comparison to pure GL, GL-HP-ßCD NF displayed improved release (46.6 ± 2.16% in 5 min) and dissolution profiles (water dissolvability ≤ 6 s). Phase solubility results showed a four-fold increase in GL solubility in GL-HP-ßCD NF. In vitro experiments on cell lines showed that inflammatory markers like IL-1ß, TNF-α, and IL-6 were significantly lower in GL-HP-ßCD NF compared to pure GL (p < 0.01 and p < 0.05). According to in vivo results, the prepared nanofiber exhibits a better anti-inflammatory effect than pure GL (63.4% inhibition vs 53.7% inhibition). The findings presented here suggested that GL-HP-ßCD NF could serve as a useful strategy for improving the therapeutic effects of GL.


Assuntos
Ácido Glicirrízico , Nanofibras , Ratos , Animais , 2-Hidroxipropil-beta-Ciclodextrina/química , Solubilidade , Ácido Glicirrízico/farmacologia , Nanofibras/química , Anti-Inflamatórios/farmacologia
8.
Nanomedicine ; 40: 102494, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34775061

RESUMO

Multidrug resistance (MDR) in cancer chemotherapy is a growing concern for medical practitioners. P-glycoprotein (P-gp) overexpression is one of the major reasons for multidrug resistance in cancer chemotherapy. The P-gp overexpression in cancer cells depends on several factors like adenosine triphosphate (ATP) hydrolysis, hypoxia-inducible factor 1 alpha (HIF-1α), and drug physicochemical properties such as lipophilicity, molecular weight, and molecular size. Further multiple exposures of anticancer drugs to the P-gp efflux protein cause acquired P-gp overexpression. Unique structural and functional characteristics of nanotechnology-based drug delivery systems provide opportunities to circumvent P-gp mediated MDR. The primary mechanism behind the nanocarrier systems in P-gp inhibition includes: bypassing or inhibiting the P-gp efflux pump to combat MDR. In this review, we discuss the role of P-gp in MDR and highlight the recent progress in different nanocarriers to overcome P-gp mediated MDR in terms of their limitations and potentials.


Assuntos
Antineoplásicos , Neoplasias , Membro 1 da Subfamília B de Cassetes de Ligação de ATP/metabolismo , Antineoplásicos/química , Antineoplásicos/farmacologia , Antineoplásicos/uso terapêutico , Resistência a Múltiplos Medicamentos , Resistencia a Medicamentos Antineoplásicos , Humanos , Neoplasias/tratamento farmacológico
9.
J Drug Deliv Sci Technol ; 76: 103764, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36090183

RESUMO

The world has witnessed an extreme vulnerability of a pandemic during 2020; originated from China. The coronavirus disease 2019 (COVID-19) is infecting and beginning deaths in thousands to millions, creating of the global economic crisis. Biosurfactants (BSs) can carry the prevention, control and management of pandemic out through diverse approaches, such as pharmaceutical, therapeutic, hygienic and environmental. The microbiotas having virulent intrinsic properties towards starting as easily as spreading of diseases (huge morbidity and mortality) could be inhibited via BSs. Such elements could be recognised for their antimicrobial activity, capability to interact with the immune system via micelles formation and in nanoparticulate synthesis. However, they can be used for developing novel and more effective therapeutics, pharmaceuticals, non-toxic formulations, vaccines, and effective cleaning agents. Such approaches can be utilized for product development and implemented for managing and combating the pandemic conditions. This review emphasized on the potentiality of BSs as key components with several ways for protecting against unknown and known pathogens, including COVID-19.

10.
AAPS PharmSciTech ; 22(1): 47, 2021 Jan 14.
Artigo em Inglês | MEDLINE | ID: mdl-33447909

RESUMO

In the last few decades, the exponential rise in the incidence of viral infections sets a global health emergency across the world. The biomimetic architecture, the ability to hijack host immune responses, continuous antigen shifting, and drafting are the major critical factors that are responsible for the unavailability of a concrete therapeutic regimen against viral infections. Further, inappropriate pharmacodynamic physicochemical and biological parameters such as low aqueous solubility, poor permeability, high affinity for plasm proteins, short biological half-lives, and fast elimination from the systemic circulation are the major critical factors that govern the suboptimal drug concentration at the target site that leads to the development of drug resistance. To address this issue, nanotechnology-based drug delivery approach is emerged as an altering method to attain the optimal drug concentration at the target site for a prolonged period by integrating the nanoengineering tools in the synthesis of nanoparticles. Nanodimensional configuration with enhanced permeability and retention effect, increased surface-area-to-volume ratio, provision for surface functionalization, etc., are the privileged aspects that make it an effective drug delivery system for dispensing the antiviral therapeutics. However, size, shape, charge, and surface topology of nanoparticles are the greater influential factors that determine target-specific drug delivery, optimum cellular uptake, degree of opsonization by the host immune cells, drug retention time, transcytosis, the extension of biological half-life, in vivo stability, and cytotoxicity. The review will enlighten the elaborative role of nanotechnology-based drug delivery and the major challenging aspect of clinical safety and efficacy.


Assuntos
Antivirais/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Nanotecnologia/métodos , Viroses/tratamento farmacológico , Animais , Antivirais/uso terapêutico , Humanos , Nanopartículas , Permeabilidade , Preparações Farmacêuticas , Solubilidade
11.
AAPS PharmSciTech ; 22(5): 164, 2021 May 26.
Artigo em Inglês | MEDLINE | ID: mdl-34041632

RESUMO

Psoriasis is a life-threatening autoimmune inflammatory skin disease, triggered by T lymphocyte. Recently, the drugs most commonly used for the treatment of psoriasis include methotrexate (MTX), cyclosporine (CsA), acitretin, dexamethasone, and salicylic acid. However, conventional formulations due to poor absorptive capacity, inconsistent drug release characteristics, poor capability of selective targeting, poor retention of drug molecules in target tissue, and unintended skin reactions restrict the clinical efficacy of drugs. Advances in topical nanocarriers allow the development of prominent drug delivery platforms can be employed to address the critical issues associated with conventional formulations. Advances in nanocarriers design, nano-dimensional configuration, and surface functionalization allow formulation scientists to develop formulations for a more effective treatment of psoriasis. Moreover, interventions in the size distribution, shape, agglomeration/aggregation potential, and surface chemistry are the significant aspects need to be critically evaluated for better therapeutic results. This review attempted to explore the opportunities and challenges of current revelations in the nano carrier-based topical drug delivery approach used for the treatment of psoriasis.


Assuntos
Portadores de Fármacos/administração & dosagem , Sistemas de Liberação de Medicamentos/tendências , Nanocápsulas/administração & dosagem , Psoríase/tratamento farmacológico , Administração Cutânea , Animais , Ciclosporina/administração & dosagem , Ciclosporina/metabolismo , Portadores de Fármacos/metabolismo , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos/efeitos dos fármacos , Liberação Controlada de Fármacos/fisiologia , Humanos , Lipossomos/administração & dosagem , Lipossomos/metabolismo , Metotrexato/administração & dosagem , Metotrexato/metabolismo , Psoríase/metabolismo , Ácido Salicílico/administração & dosagem , Ácido Salicílico/metabolismo
12.
Pharm Dev Technol ; 25(7): 797-814, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-32267180

RESUMO

Mucosa has now been recognized as a potential site for both local and systemic delivery of therapeutics. Mucoadhesive drug delivery systems with customizable release profiles have recently gained considerable interest among formulation scientists to improve clinical outcomes of drugs. This review summarizes the current development in the processing methods and polymers involved in mucoadhesive drug delivery systems. Mucoadhesive drug delivery systems are suitable for drugs that have a localized effect, undergo extensive pre-systemic metabolism, narrow absorption window, and narrow therapeutic index. Polymer characteristics like surface charge, hydrophilic surface groups, wettability, molecular weight, chain flexibility, molecular conformations, etc. are critical for assessing the extent of mucoadhesiveness and treatment response. The current review focuses on valuable principles, merits, drawbacks, and future outlooks of different mucoadhesive drug delivery systems.


Assuntos
Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Mucosa Bucal/metabolismo , Preparações Farmacêuticas/administração & dosagem , Adesividade , Animais , Vias de Administração de Medicamentos , Previsões , Humanos , Mucosa Bucal/efeitos dos fármacos , Preparações Farmacêuticas/metabolismo
13.
Pharm Dev Technol ; 25(6): 748-756, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32149557

RESUMO

The current application was aimed to evaluate the therapeutic potential of selenium and ketoconazole nanoparticles loaded hyaluronic acid gel against seborrhoeic dermatitis (SD). Amalgamation of ketoconazole (antifungal medication) and selenium (pro-oxidant) in an optimized formulation setting may help in the treatment of SD. In this study, selenium and ketoconazole nanoparticles loaded hyaluronic acid (HA) hydrogel was prepared by mechanical mixing followed by sonication. Results of the optimized batch showed a mean particle size of 121 ± 12 nm for ketoconazole and 51 ± 7 nm for selenium. SEM and TEM study revealed the prepared nanoparticles are of nanoscale dimension, with smooth spherical outline. Finally, the optimized nanoparticles were incorporated into HA hydrogel. Hydrogel exhibits desirable physical, mechanical and rheological characteristics appropriate for topical application. Optimized gel formulation exhibited an enhanced permeability with better antifungal, and anti-inflammatory activities, compared with the plain drug suspension. The optimized hydrogel with ketoconazole and selenium in nanotemplate could offer a potential strategy for the treatment of SD.


Assuntos
Dermatite Seborreica/tratamento farmacológico , Hidrogéis/administração & dosagem , Nanopartículas/administração & dosagem , Absorção Cutânea/efeitos dos fármacos , Administração Tópica , Animais , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/metabolismo , Dermatite Seborreica/metabolismo , Cabras , Células HeLa , Humanos , Hidrogéis/química , Hidrogéis/metabolismo , Cetoconazol/administração & dosagem , Cetoconazol/química , Cetoconazol/metabolismo , Masculino , Nanopartículas/química , Nanopartículas/metabolismo , Técnicas de Cultura de Órgãos , Tamanho da Partícula , Ratos , Ratos Wistar , Selênio/administração & dosagem , Selênio/química , Selênio/metabolismo , Absorção Cutânea/fisiologia , Resultado do Tratamento
14.
J Cosmet Laser Ther ; 21(6): 332-342, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31451001

RESUMO

Objective: The objective of current study to investigate the photo protective potential of synbiotic formulation comprising of prebiotic and probiotic. Methods: Selenium nanoparticles were synthesized by chemical reduction method and investigated for physical-chemical properties including morphology, physical state, and free radical scavenging potential. Selection of probiotic biomass was made on the free radical scavenging potential by using NO assay. A topical w/o emulsion-based cream was prepared with screened ingredients to achieve a stable product with optimum free radical scavenging potential. The finished product was investigated for various mechanical, physiochemical, and viscoelastic characteristics. The SPF of optimized formulation was determined in UV-stimulated Wistar rat model. Results: Results indicated that the finished product shows nanoscale feature of elemental selenium. Cream comprising of potential free radical reagent (Selenium nanoparticles with IC50 50.097 µg/ml and biomass of Lactobacillus rhamnosus have IC50 61.63 µg/ml) exhibits a SPF of 29.77. Optimized skin care formulation has desirable physiochemical and viscoelastic properties required for topical application. Histopathology and Draize test indicated the finished product does not show any sign of skin toxicity. Conclusion: Results inferred that topical formulation combining the features of selenium and probiotic biomass offer an effective alternative for the treatment of sunburn complications.


Assuntos
Queimadura Solar/terapia , Simbióticos/administração & dosagem , Administração Cutânea , Animais , Antioxidantes/administração & dosagem , Emulsões , Sequestradores de Radicais Livres/metabolismo , Lactobacillus , Nanopartículas/química , Tamanho da Partícula , Ratos , Ratos Wistar , Selênio/administração & dosagem , Higiene da Pele , Fator de Proteção Solar
15.
AAPS PharmSciTech ; 19(8): 3687-3697, 2018 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-30225779

RESUMO

Periodontitis is a common microbial infection that involves pocket formation due to the destruction of periodontal ligament. The present work is oriented to provide a holistic approach for the treatment of periodontitis comprising localized delivery of nanometric hydroxyapatite as a reinforcing filler and silver-metronidazole as periodontal pocket disinfectant adjunct to current periodontal therapy because of its broad-spectrum antimicrobial activity and low systemic toxicity. In the present work, electrospinning technique was used to prepare medicated nanofiber enriched with antibacterial-hydroxyapatite layers for dental application. The optimized formulation was characterized by SEM, FTIR, DSC, XRD, etc. Safety assessment and therapeutic potential of optimized formulation was evaluated in both in vitro and in vivo animal models. The newly synthesized complex (silver-metronidazole) exhibited higher antibacterial activity against the selected strain over the referenced silver and metronidazole. Results of in vitro studies suggested good compatibility of the metal complex with the polymer matrix. The drug release behavior from optimized formulation shows constant in vitro release behavior. Both in vitro and in vivo studies show broad-spectrum antimicrobial activity of the metal complex and demonstrate the potential of biomimetic nano-hydroxyapatite for filling periodontal defects. All these observations indicated that the above formulation could play a useful role in the treatment of periodontitis. Graphical Abstract ᅟ.


Assuntos
Antibacterianos/administração & dosagem , Nanofibras/administração & dosagem , Periodontite/tratamento farmacológico , Prata/administração & dosagem , Animais , Feminino , Humanos , Masculino , Ratos , Ratos Wistar
16.
Pharm Dev Technol ; 21(8): 951-960, 2016 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-26334961

RESUMO

Currently, one-third of the world's population is infected with tuberculosis (TB) mainly spread by inhalation of the tubercle bacilli, Mycobacterium tuberculosis. Patient non-compliance is the major reason for failure of anti-tubercular drugs (ATDs) chemotherapy due to multidrug administration for longer duration of time period. The main aim of current research study was to develop and characterize inhalable spray-dried particles for pulmonary delivery of ATDs, i.e., rifampicin (RIF) and isoniazid (INH). ATDs-loaded alginate particles were prepared by ionotropic gelation technique followed by spray drying and characterized on the basis of various evaluation parameters. Results showed that the optimized spray-dried particles were found to be spherical in shape with excellent flow properties. The drug release showed the biphasic pattern of release, i.e., initial burst (30-40% up to 4 h) followed by a sustained release pattern (90% up to 60 h). Optimized formulations exhibited lower cytotoxicity and excellent lung uptake up to 8 h. Optimized formulation also showed higher rate and extent of drug uptake by lungs due to preferential phagocytosis be macrophage. In future, alginate particles could be a promising carrier for targeted delivery of ATDs to alveolar macrophages for efficient management of TB.


Assuntos
Antituberculosos/administração & dosagem , Antituberculosos/química , Pulmão/metabolismo , Tuberculose/tratamento farmacológico , Administração por Inalação , Alginatos/química , Animais , Química Farmacêutica/métodos , Preparações de Ação Retardada/administração & dosagem , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Feminino , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Isoniazida/administração & dosagem , Isoniazida/química , Camundongos , Camundongos Endogâmicos BALB C , Mycobacterium tuberculosis/efeitos dos fármacos , Tamanho da Partícula , Rifampina/administração & dosagem , Rifampina/química
17.
Mol Pharm ; 12(11): 3839-50, 2015 Nov 02.
Artigo em Inglês | MEDLINE | ID: mdl-26436948

RESUMO

The foremost objective of the present research study was to develop and evaluate the potential of rifampicin (RIF) and isoniazid (INH) loaded spray dried nanoembedded microparticles against experimental tuberculosis (TB). In this study, RIF-INH loaded various formulations (chitosan, guar gum, mannan, and guar gum coated chitosan) were prepared by spray drying and characterized on the basis of in vitro as well as in vivo studies. Results showed that guar gum spray dried particles showed uniform size distribution with smooth surface as compare to mannan formulations. Guar gum batches exhibited excellent flow ability attributed to their optimum moisture content and uniform size distribution. The drug release showed the biphasic pattern of release, i.e., initial burst followed by a sustained release pattern. The preferential uptake of guar gum coated formulations suggested the presence and selective uptake capability of mannose moiety to the specific cell surface of macrophages. In vivo lung distribution study showed that guar gum coated chitosan (GCNP) batches demonstrated prolonged residence at the target site and thereby improve the therapeutic utility of drug with a significant reduction in systemic toxicity. Optimized drug loaded GCNP formulation has resulted in almost 5-fold reduction of the number of bacilli as compared to control group. Histopathology study also demonstrated that none of the treated groups show any evidence of lung tissue abnormality. Hence, GCNPs could be a promising carrier for selective delivery of antitubercular drugs to alveolar macrophages with the interception of minimal side effects, for efficient management of TB.


Assuntos
Antibióticos Antituberculose/farmacologia , Materiais Revestidos Biocompatíveis/química , Sistemas de Liberação de Medicamentos , Nanocápsulas , Rifampina/farmacologia , Tuberculose Pulmonar/tratamento farmacológico , Animais , Química Farmacêutica , Quitosana/química , Materiais Revestidos Biocompatíveis/administração & dosagem , Preparações de Ação Retardada , Portadores de Fármacos , Feminino , Galactanos/química , Macrófagos/citologia , Macrófagos/efeitos dos fármacos , Macrófagos/microbiologia , Mananas/química , Camundongos , Camundongos Endogâmicos BALB C , Mycobacterium/patogenicidade , Gomas Vegetais/química , Tuberculose Pulmonar/microbiologia
18.
Artigo em Inglês | MEDLINE | ID: mdl-38608132

RESUMO

Insulin is recognized as a crucial weapon in managing diabetes. Subcutaneous (s.c.) injections are the traditional approach for insulin administration, which usually have many limitations. Numerous alternative (non-invasive) slants through different routes have been explored by the researchers for making needle-free delivery of insulin for attaining its augmented absorption as well as bioavailability. The current review delineating numerous pros and cons of several novel approaches of non-invasive insulin delivery by overcoming many of their hurdles. Primary information on the topic was gathered by searching scholarly articles from PubMed added with extraction of data from auxiliary manuscripts. Many approaches (discussed in the article) are meant for the delivery of a safe, effective, stable, and patient friendly administration of insulin via buccal, oral, inhalational, transdermal, intranasal, ocular, vaginal and rectal routes. Few of them have proven their clinical efficacy for maintaining the glycemic levels, whereas others are under the investigational pipe line. The developed products are comprising of many advanced micro/nano composite technologies and few of them might be entering into the market in near future, thereby garnishing the hopes of millions of diabetics who are under the network of s.c. insulin injections.


Assuntos
Diabetes Mellitus , Insulina , Feminino , Humanos , Insulina Regular Humana , Diabetes Mellitus/tratamento farmacológico , Administração Retal , Disponibilidade Biológica
19.
Macromol Biosci ; 24(7): e2400049, 2024 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-38577905

RESUMO

Biomaterials denoting self-healing and versatile structural integrity are highly curious in the biomedicine segment. The injectable and/or printable 3D printing technology is explored in a few decades back, which can alter their dimensions temporarily under shear stress, showing potential healing/recovery tendency with patient-specific intervention toward the development of personalized medicine. Thus, self-healing injectable hydrogels (IHs) are stunning toward developing a paradigm for tissue regeneration. This review comprises the designing of IHs, rheological characterization and stability, several benchmark consequences for self-healing IHs, their translation into tissue regeneration of specific types, applications of IHs in biomedical such as anticancer and immunomodulation, wound healing and tissue/bone regeneration, antimicrobial potentials, drugs, gene and vaccine delivery, ocular delivery, 3D printing, cosmeceuticals, and photothermal therapy as well as in other allied avenues like agriculture, aerospace, electronic/electrical industries, coating approaches, patents associated with therapeutic/nontherapeutic avenues, and numerous futuristic challenges and solutions.


Assuntos
Hidrogéis , Impressão Tridimensional , Hidrogéis/química , Humanos , Cicatrização/efeitos dos fármacos , Materiais Biocompatíveis/química , Animais , Engenharia Tecidual/métodos , Injeções , Sistemas de Liberação de Medicamentos
20.
Artigo em Inglês | MEDLINE | ID: mdl-38347796

RESUMO

BACKGROUND: Head and neck infections (HNI) associated with multidrug resistance (MDR) offer several health issues on a global scale due to inaccurate diagnosis. OBJECTIVES: This study aimed to identify the bacteria and Candidal isolates and implement the silver nanoparticles green synthesized with leaf extract of Coccinia grandis (Cg-AgNPs) as a therapeutic approach against HNI pathogens. METHODS: The Cg-AgNPs were characterized by the UV-visible spectrophotometer, FT-IR analysis, Zeta particle size, Zeta potential, and field emission scanning electron microscope (FESEM) analysis to validate the synthesis of nanoparticles. Additionally, the antimicrobial activity of Cg-AgNPs was presented by the zone of inhibition (ZOI), minimum inhibitory concentration (MIC), minimum bactericidal/fungicidal concentration (MBC/MFC), and antibiofilm assay. Moreover, the cell wall rupture assay was visualized on SEM for the morphological study of antimicrobial activities, and the in-vivo toxicity was performed in a swiss mice model to evaluate the impact of Cg-AgNPs on various biological parameters. RESULTS: Different bacterial strains (Staphylococcus aureus, Acinetobacter baumannii, Klebsiella pneumoniae, and Pseudomonas aeruginosa) and Candida sp. (Candida albicans, Candida tropicalis, Candida orthopsilosis, and Candida glabrata) were identified. The MIC, MBC, and antibiofilm potential of Cg-AgNPs were found to be highest against A. baumannii: 1.25 µg/ml, 5 µg/ml, and 85.01±5.19% respectively. However, C. albicans and C. orthopsilosis revealed 23mm and 21mm of ZOI. Subsequently, the micromorphology of the cell wall rupture assay confirmed the efficacy of Cg-AgNPs, and no significant alterations were seen in biochemical and hematological parameters on the swiss mice model in both acute and subacute toxicity studies. CONCLUSION: The green synthesized Cg-AgNPs have multifunctional activities like antibacterial, anticandidal, and antibiofilm activity with no toxicity and can be introduced against the HNI pathogens.

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