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1.
J Basic Microbiol ; 63(6): 573-583, 2023 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-36720046

RESUMO

Spirulina platensis is a photosynthetic, blue-green, spiral- or bulb-shaped microalgae. Due to the presence of minerals, vitamins, pigments (carotenes, phycocyanin and chlorophyll) proteins (55%-70%), carbohydrates (15%-25%), and essential fatty acids (5%-8%), it has been used as a nutritional supplement for decades. NASA successfully employed it as a nutritional supplement for astronauts on space missions then its popularity was increased. The chemical composition of Spirulina, which is rich in vitamins, minerals, phenolics, vital fatty acids, amino acids, and pigments, can be beneficial to human health when incorporated into meals. The pharmacological effects include antibacterial, anticancer, metalloprotective, immune-stimulating, and antioxidant. It modulates immunological activities and possesses anti-inflammatory qualities by preventing mast cells from releasing histamine. Due to its high quantity of protein, carbohydrate, lipid, vital amino and fatty acids, dietary minerals and vitamins, Spirulina exerts the abovementioned benefits. In this review, up-to-date and possible biological aspects, patents applied on Spirulina and heights of confirmation are addressed, and the extent of current and future exploration is also explored.


Assuntos
Microalgas , Spirulina , Humanos , Spirulina/metabolismo , Minerais/metabolismo , Carboidratos , Ácidos Graxos/metabolismo , Vitaminas/metabolismo
2.
Discov Nano ; 19(1): 85, 2024 May 09.
Artigo em Inglês | MEDLINE | ID: mdl-38724833

RESUMO

The escalating global challenge of antimicrobial resistance demands innovative approaches. This review delves into the current status and future prospects of bioengineered metallic nanoparticles derived from natural sources as potent antimicrobial agents. The unique attributes of metallic nanoparticles and the abundance of natural resources have sparked a burgeoning field of research in combating microbial infections. A systematic review of the literature was conducted, encompassing a wide range of studies investigating the synthesis, characterization, and antimicrobial mechanisms of bioengineered metallic nanoparticles. Databases such as PubMed, Scopus, Web of Science, ScienceDirect, Springer, Taylor & Francis online and OpenAthen were extensively searched to compile a comprehensive overview of the topic. The synthesis methods, including green and sustainable approaches, were examined, as were the diverse biological sources used in nanoparticle fabrication. The amalgamation of metallic nanoparticles and natural products has yielded promising antimicrobial agents. Their multifaceted mechanisms, including membrane disruption, oxidative stress induction, and enzyme inhibition, render them effective against various pathogens, including drug-resistant strains. Moreover, the potential for targeted drug delivery systems using these nanoparticles has opened new avenues for personalized medicine. Bioengineered metallic nanoparticles derived from natural sources represent a dynamic frontier in the battle against microbial infections. The current status of research underscores their remarkable antimicrobial efficacy and multifaceted mechanisms of action. Future prospects are bright, with opportunities for scalability and cost-effectiveness through sustainable synthesis methods. However, addressing toxicity, regulatory hurdles, and environmental considerations remains crucial. In conclusion, this review highlights the evolving landscape of bioengineered metallic nanoparticles, offering valuable insights into their current status and their potential to revolutionize antimicrobial therapy in the future.

3.
Chem Biol Drug Des ; 102(2): 377-394, 2023 08.
Artigo em Inglês | MEDLINE | ID: mdl-36916008

RESUMO

Numerous nanotech arenas in therapeutic biology have recently provided a scientific platform to manufacture a considerable swath of unique chemical entities focusing on drugs. Recently, nanoparticulate drug delivery systems have emerged to deliver a specific drug to a specified site. Among all other carriers, lipids possess features exclusive to nanostructured dosage forms. The bioavailability of orally administered drugs is typically negatively affected by their poor water solubility, resulting from the unique chemical moieties introduced. Because of their unique advantages, lipid nanoparticles must become increasingly predictable as a robust delivery mechanism. The enhanced biopharmaceutical properties and significance of lipid-based targeting technologies such as liposomes, niosomes, solid lipid nanoparticles and micelles are highlighted in this review. Pharmaceutical implications of lipid nanocarriers for the transport and distribution of various therapeutic agents, such as biotechnological products and small pharmaceutical molecules, is a booming topic. Lipid nanoparticles as drug delivery systems have many appealing properties, including high biocompatibility, ease of preparation, tissue specificity, avoidance of reticuloendothelial systems, delayed drug release, scale-up feasibility, nontoxicity and targeted delivery. The use of lipid nanoparticles to enhance the transport of biopharmaceuticals is currently considered state-of-the-art. Similarly, we critically examine the upcoming guidelines that therapeutic scientists should handle.


Assuntos
Nanopartículas , Nanoestruturas , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Lipossomos , Nanopartículas/química , Nanoestruturas/química , Micelas , Lipídeos/química
4.
Chem Biol Drug Des ; 102(3): 457-470, 2023 09.
Artigo em Inglês | MEDLINE | ID: mdl-36856306

RESUMO

Multidrug resistance in breast cancer and the associated side-effects of anticancer therapies are significant hurdles in chemotherapy-based treatment. Biodegradable polymeric nano-based targeted drug delivery technologies showed tremendous advantages in targeted local delivery with limited off-targeted side effects. Therefore, there is a persistent need to develop targeted nanomedicine systems for treatment of breast cancer. The current research attempted to develop poly (lactic-co-glycolic acid) nanoparticles loaded with raloxifene by modified emulsification solvent diffusion evaporation method to improve oral bioavailability by using Taguchi design. It was observed that the optimized formulation (1:4 drug to polymer ratio) poly (lactic-co-glycolic acid) showed a mean particle size and Polydispersity index of 218 ± 23.7 nm and 0.231 ± 0.04, respectively. The entrapment efficiency was found to be 82.30% ± 1.02%. In vitro drug delivery was found to be 92.5% ± 1.48% in 40 h. The nanoparticles were to remain stable at 2°C-8°C even after 30 days. Differential scanning calorimetry and Fourier transform infrared spectroscopy characterization techniques showed that there was no interaction between the drug and excipient. Stability studies indicate that polymeric nanoparticles were stable at 2°C-8°C after 6 months. Raloxifene nanoparticles may be the most potent targeting moieties to treat highly invasive and metastatic MCF-7 breast cancer cells.


Assuntos
Neoplasias da Mama , Nanopartículas , Humanos , Feminino , Copolímero de Ácido Poliláctico e Ácido Poliglicólico , Cloridrato de Raloxifeno , Neoplasias da Mama/tratamento farmacológico , Portadores de Fármacos/química , Ácido Poliglicólico/química , Ácido Láctico/química , Tamanho da Partícula , Nanopartículas/química
5.
Adv Healthc Mater ; 12(20): e2203104, 2023 08.
Artigo em Inglês | MEDLINE | ID: mdl-36972409

RESUMO

In recent years, the development of hyaluronic acid or hyaluronan (HA) based scaffolds, medical devices, bioconjugate systems have expanded into a broad range of research and clinical applications. Research findings over the last two decades suggest that the abundance of HA in most mammalian tissues with distinctive biological roles and chemical simplicity for modifications have made it an attractive material with a rapidly growing global market. Besides its use as native forms, HA has received much interest on so-called "HA-bioconjugates" and "modified-HA systems". In this review, the importance of chemical modifications of HA, underlying rationale approaches, and various advancements of bioconjugate derivatives with their potential physicochemical, and pharmacological advantages are summarized. This review also highlights the current and emerging HA-based conjugates of small molecules, macromolecules, crosslinked systems, and surface coating strategies with their biological implications, including their potentials and key challenges discussed in detail.


Assuntos
Receptores de Hialuronatos , Ácido Hialurônico , Animais , Ácido Hialurônico/química , Substâncias Macromoleculares , Receptores de Hialuronatos/química , Mamíferos
6.
J Biomater Sci Polym Ed ; 33(2): 262-278, 2022 02.
Artigo em Inglês | MEDLINE | ID: mdl-34547214

RESUMO

Nanogels are cross-linked, nano-sized hydrogels with dimensions ranging from 20 to 200 nm. Nanogel-based nanoplatforms have proven to be an excellent choice for pharmaceutical formulations. Nanosystems have properties that are very useful in polymeric drug delivery applications, and their particular strength is that they have these nanosystemic properties and can thus merge with polymeric materials. Drug-carrier size is designed to be nano-sized in order to maintain optimal stability, resulting in more surface area and interior space. This also allows for a prolonged period of time for loaded pharmaceuticals to circulate. They can be classified by stimuli responsive or non-responsive behavior and type of linkages present in the network chains of gel structure. Nanogel can be synthesized by Photolithographic, modified pullulan, emulsion polymerization reverse microemulsion polymerization inverse miniemulsion polymerization and free radical crosslinking polymerization technique. Hybrid nanogels are different from conventional polymer nanoparticles often employed for drug administration. They can encapsulate bioactive medicines and regulate the release of such medications over time and in particular areas. The hybrid nanogels used to create a specific form of the hybrid, especially one geared towards increasing targeted drug delivery, enhance the effectiveness of ailment treatments, but perhaps the introduction of a multifunctional nanogel-based drug delivery system.


Assuntos
Sistemas de Liberação de Medicamentos , Polietilenoimina , Portadores de Fármacos , Nanogéis , Polietilenoglicóis
7.
Prog Biomater ; 10(4): 309-320, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34813041

RESUMO

Repaglinide, a member of the meglitinide class of drugs, is a new anti-diabetic agent that is utilized as an oral hypoglycemic agent. Using glyceryl monostearate, cetyl palmitate, and tristearin as lipids and poloxamer 188 as a surfactant, repaglinide-loaded solid lipid nanoparticles were created. Solid lipid nanoparticles were prepared utilizing an o/w microemulsion technique, which included the lipids glyceryl monostearate and tristearin, as well as waxes such as cetyl palmitate and the surfactant poloxamer 188. The mean particle size of the solid lipid nanoparticles formed was around 339 nm, with an entrapment efficiency of 82.20%. In-vitro release studies continued to be conducted using the dialysis bag diffusion technique. Within 12 h, the cumulative drug release was 88.4%. The results indicate that repaglinide was released more slowly from solid lipid nanoparticles made from tristearin and glyceryl monostearate in an equal ratio. Tristearin found the controlled release and extreme entrapment from other lipid carriers like glyceryl monostearate and cetyl palmitate. Differential scanning calorimetry demonstrates that repaglinide is entangled in amorphous or molecular state within solid lipid nanoparticles. SEM microscopy revealed that the produced repaglinide solid lipid nanoparticles had a spherical shape. After one month of storage at 2-8 °C, short-term stability testing revealed no significant alteration.

8.
J Biomater Sci Polym Ed ; 32(12): 1584-1597, 2021 08.
Artigo em Inglês | MEDLINE | ID: mdl-33977874

RESUMO

The contemporary research implicates the formulation and evaluation of a thermosensitive in situ nano gelling method to improve solubility and ocular residence time of flurbiprofen. This study was carried out in two phases. In the first phase, an insolubility drug has been formulated in the form of a nanoparticulate system and evaluated for its characteristics. The nanoparticles obtained demonstrated an average size array of 150 to 250 nm in diameter, up to 79.35% encapsulation efficiency, and up to 93.42% drug release throughout 2 h. In the second phase, nanoparticulate systems were dispersed in aqueous solutions of Pluronic F 127 (14%) and various concentrations of Carbopol 934 in combination to form an in situ nano gel. The prepared in situ gel was investigated for its physicochemical properties like pH, flowability, sol-gel transition temperature, gelling capacity, and rheological properties. Carbopol 934 did not significantly affect sol-gel transition temperature in optimized concentration (<0.3%) but altered gelling capacity, pH, and transparency of the formulations. In vivo resident time and eye irritation test was evaluated in the rabbit eye. In optimized in situ gelling formulation (NIGF3), approximately 95% of in vitro drug release was observed after 6 h. NIGF3 increased precorneal residence time and high concentration in aqueous humor when paralleled to flurbiprofen eye drops. Greater concentration of drug in aqueous humor was due to its improved saturation solubility of the drug, and amplified residence time was attributed to the formation of gel matrix-embedded nanoparticles. This demonstrated that in situ nano gels (NIGF3) comprehending aqueous solutions of 0.3% w/v concentrations of Carbopol 934 with Pluronic F 127 may ominously persist the residence time and mend bioavailability of a water-insoluble drug.


Assuntos
Flurbiprofeno , Animais , Sistemas de Liberação de Medicamentos , Géis , Soluções Oftálmicas , Poloxâmero , Coelhos
9.
Curr Drug Targets ; 22(16): 1901-1914, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-33494666

RESUMO

Three Dimensional (3D) printing is a promising method for quick prototyping and manufacturing of any material. It is similar to photocopy or printing, where the new materials are formed on layers (3D) like their mother component. Following its growth and advancement in the 1980s, its application in pharmaceuticals is still limited. It has become one of the most innovative and influential tools serving as a technology for developing dosage forms from the last decade. The potential of 3D printing to produce drugs for precise measurement customized to specific patients' needs has shown the possibility of developing personalized medicines to novel dosage forms. The breakthrough allows the clear perception of the dosage structures on different shapes, sizes, surfaces and the associated challenges in delivering them by using such designed conditions. There are different difficulties related to the correct utilization of 3D imprinting in the pharmaceuticals, which have a strong impact on the scope of this technology. Recent advancements in the field of 3D printing technology used in the pharmaceutical industry mainly focused on different techniques for the fabrication of different dosage forms. The Food and Drug Administration's (FDA) recent approval of the first 3D prescription highlights possibilities for 3D printing innovation in the field of pharmaceutical drug supply. This analysis assesses 3D printing advancement possibilities, particularly in the area of custom prescriptions. This technology can be regarded as the future produced on demand, low-cost solid dosage forms and helps minimize side effects due to overdose.


Assuntos
Impressão Tridimensional , Tecnologia Farmacêutica , Formas de Dosagem , Humanos , Medicina de Precisão
10.
J Biomater Sci Polym Ed ; 32(8): 1009-1023, 2021 06.
Artigo em Inglês | MEDLINE | ID: mdl-33704008

RESUMO

Luliconazole is a potential prescription candidate drug for the treatment of topical fungal infections. However, it has water solubility and skin permeability limitations. To overcome these limitations, a niosomal gel of luliconazole was formulated using Span 60, cholesterol, and chloroform to improve its bioavailability and to reduce its toxicity. Niosomes were analyzed by transmission electron microscopy (TEM) and Fourier transform infrared spectroscopy (FTIR) for morphological and spectral studies respectively. The formulations had ideal nanometric vesicle sizes, encapsulation efficiency (88.891% ± 0.0364%), Zeta potential (-40.1 mV), and storage instability was not observed. The sustained-release profile of niosomal gel was observed for up to 24 h. The highest R2 value was 0.913; the Higuchi model was considered the best fit model for the niosomal formulations. Cytotoxicity studies confirmed the biocompatibility of the niosomal gel of luliconazole. Based on the results, it can be concluded that niosomal luliconazole may enhance the activity of luliconazole against Candida albicans (C. albicans).


Assuntos
Antifúngicos , Lipossomos , Antifúngicos/farmacologia , Géis , Imidazóis , Tamanho da Partícula , Solubilidade
11.
Drug Discov Today ; 26(7): 1721-1727, 2021 07.
Artigo em Inglês | MEDLINE | ID: mdl-33745879

RESUMO

Triple-negative breast cancers (TNBCs) form a heterogeneous group of breast carcinomas that lack expression of estrogen receptor, progesterone receptor and epidermal growth factor receptor 2. In the past decade, immune checkpoint inhibitors (ICIs) have revolutionized the arena of cancer immunotherapy. Early results are now accumulating from trials involving the treatment of TNBCs with radical ICIs therapies, including combinational therapies that include ICI technologies. In this review, we provide a broad overview of the progress of immunotherapy-based treatments and discuss future opportunities for their use in TNBC.


Assuntos
Inibidores de Checkpoint Imunológico/uso terapêutico , Neoplasias de Mama Triplo Negativas/terapia , Humanos , Imunoterapia , Microambiente Tumoral
12.
J Hazard Mater ; 409: 124493, 2021 05 05.
Artigo em Inglês | MEDLINE | ID: mdl-33229259

RESUMO

Heavy metal ions (HMIs) have been mainly originated from natural and anthropogenic agents. It has become one of biggest societal issues due to their recognised accumulative and toxic effects in the environment as well as biological media. Key measures are required to reduce the risks posed by toxic metal pollutants existing in the environment. The increased research activities of HMIs detection, and use of technologies based on electrochemical detection that combine with engineered nanomaterials, is a key promising and innovative strategy that can potentially confine heavy metal poisoning. Deep understanding of the characteristics of the physicochemical properties of nanomaterials is highly required. It is also important to interpret the parameters at the nano-bio interface level that merely affect cross-interactions between nanomaterials and HMIs. Therefore, the authors outlined the state-of-the-art techniques that used engineeringly developed nanomaterials to detect HMIs in the environment. The possible novel applications of extensive and relatively low-cost HMIs monitoring and detection are discussed on the basis of these strengths. Finally, it is concluded by providing gist on acquaintance with facts in the present-day scenario along with highlighting areas to explore the strategies to overcome the current limitations for practical applications is useful in further generations of nano-world.

13.
J Biomater Sci Polym Ed ; 32(4): 477-487, 2021 03.
Artigo em Inglês | MEDLINE | ID: mdl-33226893

RESUMO

Nitazoxanide (NTZ) is a synthetic form of nitrothiazole with a broad range of applications as an antiparasitic, antibacterial and antiviral agent. NTZ is a highly low aqueous soluble drug which possesses solubility of 0.00755 mg/mL and typically low bioavailability of 1%. Low aqueous solubility is usually regarded as prime prerequisites for enhanced absorption and bioavailability. The purpose of this study is to improve in vitro dissolution of the poorly soluble drug NTZ through amorphous solid dispersion technology. Three solid dispersions of NTZ were successfully prepared by hot-melt technique. It was further evaluated for drug content, DSC, XRD, SEM, TEM, FT-IR, in-vitro drug release study, in vitro MTT safety on HEK-293 and A-549 and stability study. The results of XRD showed after the formation of solid dispersions. The number of crystalline peaks has disappeared and confirmed the amorphous form of the drug. An in vitro release study showed that NTZ effectively released from solid dispersion into a simulated gastric releasing medium (pH 1.2). Further, the cytotoxicity study gave an indication of safe for human. Also, stability studies depicted no evident difference in the physical state of solid dispersion after six months. Hence, it can be concluded that the newly developed formulation was found to be safe and stable with enhanced solubility profile.


Assuntos
Preparações Farmacêuticas , Varredura Diferencial de Calorimetria , Portadores de Fármacos , Células HEK293 , Humanos , Nitrocompostos , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Tiazóis
14.
J Control Release ; 327: 500-511, 2020 11 10.
Artigo em Inglês | MEDLINE | ID: mdl-32858073

RESUMO

To cater to medication needs in the future healthcare system, we need to shift from the conventional system of drug delivery to modern molecular signature-based drug delivery systems. The current drug therapies are either less effective, ineffective, or produce numerous adverse reactions. One scientific principle or discipline cannot adequately address all the problems, so we need an innovative application of the current scientific principles. Here we are proposing a novel concept of nanoformulation based on pharmacogenomics and theranostics for personalized error-free and targeted therapeutic agent delivery. The addition of more knowledge about the human genome opens the new way to study disease-gene, gene-drug, and drug-effect interactions, which is the basis of future medicines. Pharmacogenomics provides information about the disease etiology, role in genes in disease pathophysiology, disease biomarkers, drug targets, drug effects, and the fate of drugs inside the body. Theranostics approach utilizes the above information in diagnosis, treatment, and monitoring of the disease on a real-time basis. Personalized dosage forms can be formulated into a nanoformulation that provides a better therapeutic effect and minimizes adverse drug reactions. The therapeutic system needs to be shifted from the principle of one drug fits all to one drug unique population. In the present manuscript, we tried to conceptualize a modern therapeutic system by combining the three approaches viz. pharmacogenomics, theranostics, and nanotechnology applied in the area of formulation development to produce a multifunctional single tiny entity.


Assuntos
Preparações Farmacêuticas , Farmacogenética , Humanos , Nanotecnologia , Medicina de Precisão
15.
Heliyon ; 6(11): e05459, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33241144

RESUMO

The paper aimed to progress an ideal gastro retentive drug delivery system intended for directing Losartan and Hydrochlorothiazide as a fixed-dose combination for anti-hypertensive therapy. The bilayer tablets were primed through direct compression method. Losartan was formulated by means of a floating layer expending hydrophilic swellable polymer Hydroxy Propyl Methyl Cellulose K4M, ethyl cellulose (4cps) as a buoyancy enhancer, sodium bicarbonate as a gas spawning agent. The amount of polymer blends remains optimized using 23 full factorial designs. The clout of experimental factors such as swelling agent concentration, buoyancy enhancer and gas generating agent on floating lag time, total floating time, T50% and % drug release remain investigated to get optimized formulation. The responses remain analyzed using Analysis of variance, and polynomial equation stood created for every retort using Multiple linear regression analysis. Entirely preparations floated for more than 12 h. The release pattern of losartan stood fitted to diverse models based on the coefficient of correlation (r). All the formulations, except F2, showed the Korsemeyer-Peppas model as the best fit model. Formulation F2 showed the zero-order model. Diffusion exponents (n) remained indomitable designed for entirely formulations (0.45-0.89), accordingly the chief drug discharge mechanism was non-fickian (anamolous) transport. Formulation F4 containing 20% w/w Hydroxy Propyl Methyl Cellulose K4M, 15% Sodium bicarbonate and 5% ethyl cellulose (4cps) was the best formulation as per the range of drug release remain institute to be more than 95 % in 12h and floating lag time was 20.15 s. The immediate-release layer stood optimized using crospovidone and Indion 414 as a super disintegrant. Formulation A8 containing 2% Indion 414 was considered as optimized formulation as it released 99% drug within 35 min and possessed less disintegration time. Optimized formulation F4 from the controlled-release layer and A8 from immediate-release layer was used to formulate bilayer tablet. The optimized formulation was imperilled to stability reading for three months at 40○C/75% relative humidity. The stability revision exhibited no substantial alteration in the appearance of tablets, floating characteristics, drug content and in-vitro drug dissolution. Consequently, a biphasic drug release design was effectively accomplished over the formulation of floating bilayer tablets.

16.
Int J Nanomedicine ; 11: 1089-95, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27051284

RESUMO

The aim of this study was to develop a novel microbially triggered and animal-sparing dissolution method for testing of nanorough polysaccharide-based micron granules for colonic drug delivery. In this method, probiotic cultures of bacteria present in the colonic region were prepared and added to the dissolution media and compared with the performance of conventional dissolution methodologies (such as media with rat cecal and human fecal media). In this study, the predominant species (such as Bacteroides, Bifidobacterium, Lactobacillus species, Eubacterium and Streptococcus) were cultured in 12% w/v skimmed milk powder and 5% w/v grade "A" honey. Approximately 10(10)-10(11) colony forming units m/L of probiotic culture was added to the dissolution media to test the drug release of polysaccharide-based formulations. A USP dissolution apparatus I/II using a gradient pH dissolution method was used to evaluate drug release from formulations meant for colonic drug delivery. Drug release of guar gum/Eudragit FS30D coated 5-fluorouracil granules was assessed under gastric and small intestine conditions within a simulated colonic environment involving fermentation testing with the probiotic culture. The results with the probiotic system were comparable to those obtained from the rat cecal and human fecal-based fermentation model, thereby suggesting that a probiotic dissolution method can be successfully applied for drug release testing of any polysaccharide-based oral formulation meant for colonic delivery. As such, this study significantly adds to the nanostructured biomaterials' community by elucidating an easier assay for colonic drug delivery.


Assuntos
Colo/efeitos dos fármacos , Portadores de Fármacos/farmacocinética , Sistemas de Liberação de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos/métodos , Nanoestruturas/química , Animais , Meios de Cultura/química , Portadores de Fármacos/administração & dosagem , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Fezes/microbiologia , Fluoruracila/administração & dosagem , Galactanos/química , Humanos , Mananas/química , Gomas Vegetais/química , Ácidos Polimetacrílicos , Polissacarídeos/química , Probióticos , Ratos , Solubilidade
17.
Int J Pharm Investig ; 6(2): 116-22, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27051631

RESUMO

INTRODUCTION: Oral sustained release gastro retentive dosage forms offer several advantages for drugs having absorption from the upper gastrointestinal tract to improve the bioavailability of medications which have narrow absorption window. The aim of the study was to develop a floating bioadhesive drug delivery system exhibiting a unique combination of floatation and bioadhesion to prolong the residence in the stomach using atenolol as a model drug. METHODS: Prior to compression, polymeric blend(s) were evaluated for flow properties. The tablets were prepared by direct compression method using bioadhesive polymer like Carbopol 934P and hydrophilic polymers like HPMC K4M, HPMC K15M, and HPMC K100M. The prepared tablets were evaluated for physical characteristics, bioadhesive strength, buoyancy lag time, swelling index and in vitro drug release studies. RESULTS: The mean bioadhesive strength was found to be in the range of 16.2 to 52.1 gm. The optimized blend (F11) showed 92.3% drug releases after 24 hrs. Whilst, increase in concentration of carbopol 934P, bioadhesive strength and swelling index was increased with slow release. The n values of optimized formulations were found in the range of 0.631-0.719 indicating non-fickian anomalous type transport mechanism. CONCLUSION: The study aided in developing an ideal once-a-day gastro retentive floating drug delivery system with improved floating, swelling and bioadhesive characteristics with better bioavailability.

18.
Int J Nanomedicine ; 11: 1475-82, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27114707

RESUMO

Transdermal drug delivery systems have made significant contributions to the medical community, but have yet to completely substitute oral or parenteral delivery. Recently, various strategies have been used to augment the transdermal delivery of therapeutics. Primarily, they include iontophoresis, electrophoresis, sonophoresis, chemical permeation enhancers, microneedles, and vesicular systems. Among these strategies, elastic liposomes appear promising. Elastic vesicle scaffolds have been developed and evaluated as novel topical and transdermal delivery systems, with an infrastructure consisting of hydrophobic and hydrophilic moieties together, and as a result, such scaffolds can accommodate drug molecules with a wide range of solubility. High deformability of these vesicles provides for better penetration of intact vesicles. This system is much more efficient at delivering low- and high-molecular-weight drugs to the skin in terms of quantity and depth. In this work, elastic liposomes of Tramadol HCl were prepared using a solvent evaporation method with different surfactants and were characterized using microscopy, and particle size, shape, drug content, ex vivo release, and zeta potential were also calculated. The prepared elastic liposomes were found to be in the range of 152.4 nm with a zeta potential of -22.4 mV; the entrapment efficiencies of the selected formulation was found to be 79.71%±0.27%. All formulations in the form of a gel were evaluated for physicochemical properties and were found to be homogeneous with no grittiness, and the pH of all formulations was found to be neutral. The optimized selected elastic liposomal formulation followed the Higuchi equation and Fickian diffusion and released the drug for a period of 24 hours. The overall results provide much promise for the continued investigation of deformable vesicles as transdermal drug carriers.


Assuntos
Analgésicos Opioides/farmacologia , Composição de Medicamentos , Géis/administração & dosagem , Lipossomos/química , Pele/efeitos dos fármacos , Tensoativos/química , Administração Cutânea , Analgésicos Opioides/administração & dosagem , Analgésicos Opioides/química , Animais , Química Farmacêutica , Portadores de Fármacos/metabolismo , Elasticidade , Excipientes , Géis/química , Interações Hidrofóbicas e Hidrofílicas , Tamanho da Partícula , Ratos , Absorção Cutânea , Solubilidade
19.
Int J Nanomedicine ; 10: 7175-82, 2015.
Artigo em Inglês | MEDLINE | ID: mdl-26648721

RESUMO

Targeted drug delivery plays a significant role in disease treatment associated with the colon, affording therapeutic responses for a prolonged period of time with low side effects. Colorectal cancer is the third most common cancer in both men and women with an estimated 102,480 cases of colon cancer and 40,340 cases of rectal cancer in 2013 as reported by the American Cancer Society. In the present investigation, we developed an improved oral delivery system for existing anticancer drugs meant for colon cancer via prebiotic and probiotic approaches. The system comprises three components, namely, nanoparticles of drug coated with natural materials such as guar gum, xanthan gum (that serve as prebiotics), and probiotics. The natural gums play a dual role of protecting the drug in the gastric as well as intestinal conditions to allow its release only in the colon. In vitro results obtained from these experiments indicated the successful targeted delivery of 5-fluorouracil to the colon. Electron microscopy results demonstrated that the prepared nanoparticles were spherical in shape and 200 nm in size. The in vitro release data indicated that the maximum release occurs at pH 7.2 and 7.4 with 93% of the drug released in the presence of 4% (w/v) of rat cecal content. In vivo results conclude a practical mechanism to maintain the integrity and intactness of the intestinal/colonic microflora, in the face of a "chemical attack" by oral colon-targeted drug delivery for colon cancer treatment.


Assuntos
Colo/efeitos dos fármacos , Sistemas de Liberação de Medicamentos/métodos , Fluoruracila/administração & dosagem , Fluoruracila/farmacologia , Nanomedicina/métodos , Animais , Peso Corporal/efeitos dos fármacos , Ceco/metabolismo , Colo/patologia , Diarreia/diagnóstico , Liberação Controlada de Fármacos , Feminino , Humanos , Masculino , Nanopartículas/química , Nanopartículas/ultraestrutura , Ratos Wistar
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