Performance evaluation of PAMAM dendrimer based simvastatin formulations

Kulhari, Hitesh; Pooja, Deep; Prajapati, Sunil; Chauhan, Abhay Singh

doi:10.1016/j.ijpharm.2010.12.002

Cited by 100 publications

(44 citation statements)

References 30 publications

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“…Dendrimers represents a versatile nanocarrier for chemists towards fabrication of siRNA/miRNA nanoformulations with amendable terminal structure to attain prolonged circulatory lifetime, sustained release of bioactives and targeting potential [177, 178]. Also the dendrimers have a higher loading capacity for the delivery of the drugs into tumor tissues.…”

Section: Nanotechnology Based Approaches To Deliver Rnai Based Commentioning

confidence: 99%

Nanocarrier mediated delivery of siRNA/miRNA in combination with chemotherapeutic agents for cancer therapy: Current progress and advances

Gandhi

Tekade

Chougule

2014

Journal of Controlled Release

336

270

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Chemotherapeutic agents have certain limitations when it comes to treating cancer, the most important being severe side effects along with multidrug resistance developed against them. Tumor cells exhibits drug resistance due to activation of various cellular level processes viz. activation of drug efflux pumps, anti-apoptotic defense mechanisms etc. Currently, RNA interference (RNAi) based therapeutic approaches are under vibrant scrutinization to seek cancer cure. Especially small interfering RNA (siRNA) and micro RNA (miRNA), are able to knock down the carcinogenic genes by targeting the mRNA expression, which underlies the uniqueness of this therapeutic approach. Recent research focus in the regime of cancer therapy involves the engagement of targeted delivery of siRNA/miRNA in combinations with other therapeutic agents (such as gene, DNA or chemotherapeutic drug) for targeting permeability glycoprotein (P-gp), Multidrug resistant protein 1(MRP-1), B-cell lymphoma (BCL-2) and other targets that are mainly responsible for resistance in cancer therapy. RNAi-chemotherapeutic drug combinations have also been found to be effective against different molecular targets as well and can increase the sensitization of cancer cells to therapy several folds. However, due to stability issues associated with siRNA/miRNA suitable protective carrier is needed and nanotechnology based approaches have been widely explored to overcome these drawbacks. Furthermore, it has been univocally advocated that the co-delivery of siRNA/miRNA with other chemodrugs significantly enhances their capability to overcome cancer resistance compared to naked counterparts. The objective of this article is to review recent nanocarrier based approaches adopted for the delivery of siRNA/miRNA combinations with other anticancer agents (siRNA/miRNA/pDNA/chemodrugs) to treat cancer.

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Section: Nanotechnology Based Approaches To Deliver Rnai Based Commentioning

confidence: 99%

Nanocarrier mediated delivery of siRNA/miRNA in combination with chemotherapeutic agents for cancer therapy: Current progress and advances

Gandhi

Tekade

Chougule

2014

Journal of Controlled Release

336

270

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“…The obtained data were used for the analysis of any physical or chemical degradation at specified storage conditions at 4°C (Kulhari et al 2011).…”

Section: Physical Stability Studiesmentioning

confidence: 99%

p-Hydroxy benzoic acid-conjugated dendrimer nanotherapeutics as potential carriers for targeted drug delivery to brain: an in vitro and in vivo evaluation

et al. 2015

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Dendrimers which are discrete nanostructures/nanoparticles are emerging as promising candidates for many nanomedicine applications. Ligandconjugated dendrimer facilitate the delivery of therapeutics in a targeted manner. Small molecules such as p-hydroxyl benzoic acid (pHBA) were found to have high affinity for sigma receptors which are prominent in most parts of central nervous system and tumors. The aim of this study was to synthesize pHBA-dendrimer conjugates as colloidal carrier for site-specific delivery of practically water insoluble drug, docetaxel (DTX) to brain tumors and to determine its targeting efficiency. pHBA, a small molecule ligand was coupled to the surface amine groups of generation 4-PAMAM dendrimer via a carbodiimide reaction and loaded with DTX. The conjugation was confirmed by 1 HNMR and FT-IR spectroscopy. In vitro release of drug from DTXloaded pHBA-conjugated dendrimer was found to be less as compared to unconjugated dendrimers. The prepared drug delivery system exhibited good physico-chemical stability and decrease in hemolytic toxicity. Cell viability and cell uptake studies were performed against U87MG human glioblastoma cells and formulations exerted considerable anticancer effect than plain drug. Conjugation of dendrimer with pHBA significantly enhanced the brain uptake of DTX which was shown by the recovery of a higher percentage of the dose from the brain following administration of pHBA-conjugated dendrimers compared with unconjugated dendrimer or formulation in clinical use (Taxotere Ò ). Therefore, pHBA conjugated dendrimers could be an efficient delivery vehicle for the targeting of anticancer drugs to brain tumors.

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“…As it can be seen from these data the higher dynamic release According to Massaro et al [44] the basic equation of mass uptake by polymer material is given by Equation (7). where n exponent is the type of diffusion mechanism and k is the constant which depends on diffusion coefficient and film thickness. By analogy with equation (3) n = 0.5 and k takes the following expression (8) As it can be seen from the D and k values reported in Table 3 that the diffusion rate slightly decreased as the pH media increased, thus indicating a very low influence of the pH-media on the swelling process.…”

Section: In Vitro Study Of Folic Acid Releasedmentioning

confidence: 94%

“…Indeed, according to different investigations, the smaller the FA particle size, the higher the solubility. [3][4][5][6][7][8] In this work, the maximum concentration of FA is deduced from the FA released at 37 °C in different pH media during one week. Noting that, at the end of the release process, only FA was deposed in the bottom of the Becker after removing the specimen and total evaporation of media.…”

Section: Solubility Enhancement Of Fa In Watermentioning

confidence: 99%

“…Indeed, according to different investigators, the smaller the drug particles size, the higher is the solubility. [3][4][5][6][7][8] Solid dispersion method has also been employed by different investigators to increase the drug-water solubility. This technique applied on sulfathiazole [9] and chloramphenicol [10] by Sekiguchi led to promising results.…”

Section: Introductionmentioning

confidence: 99%

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Poly(2-hydroxyethylmethacrylate-graft-folic acid), synthesis, solubility enhancement, and release dynamic of folic acid

Beagan

Aouak

AlJuhaiman

et al. 2016

Designed Monomers and Polymers

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A series of poly (2-hydroxyethylmethacrylate-graft-folic acid) (FAHEMA) systems are synthesized by grafting of folic acid (FA) into poly (2-hydroxyethylmethacrylate) via an esterification reaction. The structure of these copolymers is confirmed by NMR and CHN analyses. The thermal behavior of these materials is characterized by DSC and TGA analyses. The surface morphology of FAHEMA films before and after the release process is examined by the SEM method. The cumulative FA released in different pH media from FAHEMA materials occurred via a retro-esterification reaction at body temperature during 72 h in which the influence of the swelling degree of PHEMA, the FA content and pH media on the dynamic release is widely investigated. The results obtained revealed that the solubility of FA in water deduced from the release process is widely improved compared with literature reports. It is also revealed that the diffusion of water in different pH media through the PHEMA matrix and that of FA through FAHEMA materials perfectly obeyed the Fickian models. It was deduced from the kinetic study that the release performance is obtained with the copolymers containing initially 10 and 20 wt% of FA contents.

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Performance evaluation of PAMAM dendrimer based simvastatin formulations

Cited by 100 publications

References 30 publications

Nanocarrier mediated delivery of siRNA/miRNA in combination with chemotherapeutic agents for cancer therapy: Current progress and advances

Nanocarrier mediated delivery of siRNA/miRNA in combination with chemotherapeutic agents for cancer therapy: Current progress and advances

p-Hydroxy benzoic acid-conjugated dendrimer nanotherapeutics as potential carriers for targeted drug delivery to brain: an in vitro and in vivo evaluation

Poly(2-hydroxyethylmethacrylate-graft-folic acid), synthesis, solubility enhancement, and release dynamic of folic acid

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