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BACKGROUND: Global cancer statistics defines the severity of disease even after significant research worldwide. PROBLEM: Failure of the currently available treatment approaches, including surgery, radiation therapy and traditional chemotherapy. AIM: The aim of this review is to discuss the role of phytochemical based nano-formulations for treatment of cancer. DISCUSSION: In the past few decades, phytochemicals have gained popularity for acting as a potential anticancer treatment with low systemic toxicity, especially in terms of cell cycle control and cancer cell killing. Natural resources, with their immense structural variety, serve as a vital source of fresh, therapeutically useful new chemical entities for the treatment of cancer. Vinca alkaloids (VCR), vinblastine, vindesine, vinorelbine, taxanes (PTX), podophyllotoxin and its derivatives (etoposide (ETP), teniposide, camptothecin (CPT) and its derivatives (topotecan, irinotecan), anthracyclines (doxorubicin, daunorubicin, epirubicin, idarubicin, as natural products or their derivatives account for half of all anticancer drugs approved worldwide, and they have been developed utilising the knowledge learned from the natural small molecules or macromolecules. Trabectedin, an epothilone derivative, ixabepilone, and temsirolimus, three new anticancer medications launched in 2007, were derived from microbial origins. Current therapy regimens require selective drug targeting to enhance efficacy against cancer cells while normal cells remain unharmed. Modified medications and systems for drug delivery based on nanotechnology are in the process of being explored and launched in the industry for enhanced therapy and management of cancer, along with promising outcomes. Many obstacles related to cancer cell drug delivery can be overcome by using nano-particulate drug carriers, including enhancing the stability and solubility of the drug, prolonging half-lives of the drug in the blood, decreasing side effects to undesired organs, and increasing medication concentration at the desired site. The scientific initiatives and studies concerning the use of nanotechnology for some selective compounds derived from plants are discussed in this review article. CONCLUSION: The present review highlights the phytochemical-based nanoformulations and their strategies in the development of novel systems of drug delivery such as nano-liposomes, functionalized nanoparticles (NPs), and polymer nano-conjugates, SNEDDS (Self nano emulsifying drug delivery system) as this review paper depicts, as well as their rewards over conventional systems of drug delivery, as evidenced by improved biological activity depicted in their in vitro and in vivo anticancer assays.
Subject(s)
Antineoplastic Agents , Nanoparticles , Neoplasms , Humans , Drug Delivery Systems , Neoplasms/drug therapy , Drug Carriers/chemistry , Phytochemicals/therapeutic useABSTRACT
PURPOSE: In the present study rapid melt tablets (RMT's) of carvedilol were prepared by using ionotropic-gelated chitosan nanoparticles using a spray-drying method. Carvedilol is beta-adrenergic antagonist and its oral bioavailability is about 25-35% because of first pass metabolism. METHODS: The spray-dried microparticles were formulated into RMT's using a wet granulation process. The Formulation and optimization of carvedilol loaded RMTs using nano and microparticulate chitosan based system (NMCS) was done by using 32 factorial designs. RESULTS: Drug entrapment efficiency of about 64.9 % (w/w) and loading capacity of 14.44% (w/w) were achieved for the microparticles, which were ranged from 1 µm to 4 µm in diameter. RESULTS of disintegration tests showed that the formulated RMTs could be completely dissolved within 40 seconds. Dissolution studies suggested that Carvedilol is released more slowly from tablets made using the microencapsulation process compared with tablets containing Carvedilol that is free or in the form of nanoparticles. CONCLUSION: RESULTS shown that the development of new RMTs designed with crosslinked microparticle might be a rational way to overcome the unwanted taste of conventional RMTs and the side effects related to Carvedilol intrinsic characteristics. The development of Carvedilol NMCS using ludiflash as RMTs could be used as a promising approach for improving the solubility and oral bioavailability of water insoluble drug.
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The use of nanotechnology based on the development and fabrication of nanostructures is one approach that has been employed to overcome the challenges involved with conventional drug delivery systems. Formulating Nanoplex is the new trend in nanotechnology. A nanoplex is a complex formed by a drug nanoparticle with an oppositely charged polyelectrolyte. Both cationic and anionic drugs form complexes with oppositely charged polyelectrolytes. Compared with other nanostructures, the yield of Nanoplex is greater and the complexation efficiency is better. Nanoplex are also easier to prepare. Nanoplex formulation is characterized through the production yield, complexation efficiency, drug loading, particle size and zeta potential using scanning electron microscopy, differential scanning calorimetry, X-ray diffraction and dialysis studies. Nanoplex have wide-ranging applications in different fields such as cancer therapy, gene drug delivery, drug delivery to the brain and protein and peptide drug delivery...
O uso da nanotecnologia baseada no desenvolvimento e na fabricação de nanoestruturas é uma abordagem que tem sido empregada para superar os desafios envolvidos nos sistemas de liberação de fármacos convencionais. A formulação de nanoplexos é a nova tendência na nanotecnologia. Um nanoplexo é um complexo formado pela nanopartícula do fármaco com poplieletrólito de carga oposta. Tanto fármacos catiônicos quanto aniônicos formam complexos com polieletrólitos opostamente carregados. Comparado com outras nanoestruturas, o rendimento dos nanoplexos é maior e a eficiência de complexação é melhor. Nanoplexos são, também. De mais fácil preparação. A formulação de nanoplexo é caracterizada pelo rendimento de produção, eficiência de complexação, carga do fármaco, tamanho de partícula e potencial zeta, utilizando microscopia eletrônica de varredura, calorimetria exploratória diferencial, difração de raios X e estudos de diálise. Os nanoplexos têm aplicações amplas em diferentes campos, como terapia antineoplásica, liberação em terapia gênica, liberação cerebral de fármaco, liberação de fármacos protéicos e peptídicos...
Subject(s)
Humans , Drug Compounding , Nanotechnology , Nanoparticles/chemistry , Chemistry, PharmaceuticalABSTRACT
PURPOSE: In the present study, we have formulated zaltoprofen loaded, surface decorated, biodegradable gelatin nanogel and evaluated its texture characterization. METHODS: The method used to prepare gelatin nanoparticles (GNP) was 'two step desolvation' and its surface decoration was performed with oleic acid (OA). The GNP was optimized by DOE software. Nanogels were evaluated for particle size entrapment efficiency, texture properties, SEM, in-vitro, ex-vivo drug release studies, in-vitro characterization, stability and in vivo evaluation of nanogel for anti-inflammatory activity was carried out by carrageenan induced rat paw edema method as an anti-inflammatory experimental model. RESULTS: The formulated GNP with particle size and entrapment efficiency of optimized batch was found to be 247.1 nm and 76.21% respectively. The SEM of GNP shows smooth and spherical shape. In-vitro and Ex-vivo drug release shows that there was 69.47% and 78.59% drug released within 48 hrs. It follows Ritger peppas model, which indicates sustained drug release. The good texture properties of nanogel were observed from texture analysis graphs.In vivo studies of our formulation give significant results compared to the marketed nanogel. Stability data revealed stability of nanogel formulation up to 3 months. CONCLUSION: The present approach can provide us promising results of the sustained analgesic activity and the stability of drug within the GNP.
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PURPOSE: The objective of this work was to develop a bioadhesive topical gel of sertaconazole nitrate with the help of response-surface approach. METHODS: Experiments were performed according to a 3-level factorial design to evaluate the effects of two independent variables [amount of Carbapol 934 = X1) and Sodium carboxymethylcellulose (NaCMC) = X2)] on the bioadhesive character of gel, rheological property of gel (consistency index), and in-vitro drug release. The best model was selected to fit the data. RESULTS: Mathematical equation was generated by Design Expert® software for the model which assists in determining the effect of independent variables. Response surface plots were also generated by the software for analyzing effect of the independent variables on the response. The effect of formulation variables on the product characteristics can be easily predicted and precisely interpreted by using a 3-level factorial design and generated quadratic mathematical equations. CONCLUSION: On the basis of product characteristics viscosity, bioadhesiveness, permeation study, in-vitro release, in-vivo studies, TPA and spreadability it can be concluded that the best batch of topical bioadhesive gel of Sertaconazole nitrate would be with 1% Carbopol 934 and 1% NaCMC.
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In the present investigation, pulsatile release beads were prepared by ionic gelation technique. Lornoxicam dual cross-linked beads were prepared by dropping dispersed phase of lornoxicam, pectin, and sodium alginate into the dispersion phase of different concentrations of calcium chloride solution followed by aluminium chloride solution. The formulated beads were further coated by Eudragit L & S 100 in the ratio 1 : 2 w/w in order to achieve desired lag time. In vitro release study showed lag time of 5-8 h before release of lornoxicam from the formulated beads. Thus, formulated dual cross-linked beads when administered at bed time may release lornoxicam when needed most for chronotherapeutics of early morning rheumatoid arthritis attacks in chronic patients.
