Now a day's natural polymer based nanoparticulate system have been widely studied as particulate vehicles in the bio-medical and pharmaceutical area. Alginate, a natural biopolymer show good ...biodegradability, biocompatibility and non toxic, has received attention to utilise as a carrier for preparation of polymeric nanoparticles. Chemically and physically alginate can modified easily and obtained various structure having various properties, and versatile applications. Various properties and structure such as biodegradability, gelling property, mechanical strength and cell affinity can be obtained through combination of alginate with other biopolymers, immobilization of specific molecules such as sugar molecules and peptide through chemical or physical cross-linking.
In this article, we report different method of preparation of alginate nanoparticles, and also focus on recent advances of nanoparticles made of alginate and its modified form in the field of drug delivery applications.
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•Propylation of karaya gum led to the formation of self-assembled nanogels in water.•Low CAC and high zeta potential indicated physical stability of nanogels.•Core-shell nanogels ...accommodated more than 85% bosentan in hydrophobic core.•Nanogels exhibited pH-sensitive drug release behavior in simulated bio-fluids.•Pre-clinical testing demonstrated prolonged anti-hypertensive activity.
The amphiphilic propyl Karaya gum (KG) with a degree of propyl group substitution of 3.24 was synthesized to design self-assembled nanogels as carriers for bosentan monohydrate, a poorly soluble antihypertensive drug. The drug was physically hosted into the hydrophobic core of the micellar nanogels by solvent evaporation method. TEM images revealed spherical shape and core-shell morphology of the nanogels. Depending upon polymer: drug weight ratio, the drug entrapment efficiency of >85% was attained. The carriers had hydrodynamic diameter in the range of 230–305 nm with narrow size distribution. The zeta potential of −23.0 to −24.9 mV and low critical association concentration (CAC) of 8.32 mg/l provided evidence that the colloidal nanogel system was physically stable. Thermodynamics of the propyl KG system in water favored spontaneous self-assembly of propyl KG. FTIR, thermal and x-ray analyses suggested that the drug was compatible in the hydrophobic confines of the nanogels. The micellar nanogels liberated their contents in simulated gastrointestinal condition in a pH-dependent manner over a period of 10 h. Peppas-Sahlin modeling of in vitro drug release data suggested that the polymer relaxation/swelling mechanism dominated the drug release process. Pre-clinical testing of the mucoadhesive nanogel formulations exhibited that the system could monitor the anti-hypertensive activity for a prolonged period. Overall, this propyl KG micellar nanogel system had a great potential and splendid outlook to serve as novel oral controlled release carriers for poorly soluble drugs with outstanding pharmacodynamics.
•Alprazolam-loaded nanoparticles for oral use were prepared by heat coagulation.•Chitosan, egg albumin and PEG 400 were used as excipients.•Among them, highest drug entrapment was found ...99.37±4.86%.•The highest drug entrapped nanoparticles showed average particle size of 259.60nm.•The in vitro drug release showed sustained drug release over 24h.
The possibility of inter-polymeric complexation of cationic chitosan and anionic egg albumin stabilized with PEG 400 to develop novel nanoparticles for oral delivery of alprazolam by heat coagulation method at pH 5.4 and 80°C. Nine formulations were prepared by changing the concentration of chitosan, PEG 400 and heating time. The alprazolam entrapment efficiency of these nanoparticles was in the range of 68.12±1.27 to 99.37±4.86%. These nanoparticles were characterized by FTIR, DSC, P-XRD and FE-SEM analysis. Average particle diameter, poly-dispersity index and zeta potential of these nanoparticles were found 259.60nm, 0.501, and −9.00mV, respectively. The in vitro drug release from these alprazolam-loaded nanoparticles showed sustained drug release over a period of 24h. In conclusion, these newly developed chitosan-egg albumin-PEG nanoparticles were found to be a promising vehicle for sustained release delivery of lipophilic drugs.
The present review aims to highlight the applications of thermoresponsive polymers. Thermo-responsive polymers show a sharp change in properties upon a small or modest change in temperature. This ...behaviour can be utilized for the preparation of so-called ‘smart’ drug delivery systems, which mimic biological response behaviour to a certain extent. Such materials are used in the development of several applications, such as drug delivery systems, tissue engineering scaffolds and gene delivery. Advances in this field are particularly relevant to applications in the areas of regenerative medicine and drug delivery. This review addresses summary of the main applications of thermoresponsive polymers which are categorized based on their 3-dimensional structure; hydrogels, interpenetrating networks, micelles, films and particles. The physico-chemical behaviour underlying the phase transition is also discussed in brief.
OBJECTIVE: The objective of the study was to characterize the mechanism associated with metabolic syndrome (MetS)-associated cognitive decline and determine the effect of minocycline on the above ...condition in mice.
MATERIALs AND METHODS: We developed a HFHC diet-induced MetS model in mice. Diagnostic characteristics of MetS including waist circumference, lipid levels, blood pressure, and fasting blood glucose were measured in these Swiss albino mice. Cognitive parameters were measured using passive avoidance and elevated plus maze test. Hippocampal acetylcholine esterase (AchE), reduced glutathione (GSH), and cytokine levels were measured and histopathological evaluation conducted. The MetS animals were administered minocycline (50 mg/kg; 10 days) and the above parameters were measured.
RESULTS: We successfully induced MetS using HFHC diet in mice. Animals showed significantly higher fasting blood glucose levels (P < 0.001), systolic blood pressure (P < 0.01), waist circumference (P < 0.001), low-density lipoprotein (P < 0.001), and triglyceride (P < 0.01) and reduced high density lipoprotein levels (P < 0.05) compared to control animals. Both scopolamine and MetS significantly lowered (P < 0.01) step-down latency and increased transfer latency (P < 0.001). MetS animals showed significantly higher AchE (P < 0.001) and tumor necrosis factor-α (P < 0.001) and Interleukin-1 β (P < 0.01) and lower GSH (P < 0.001) levels and reduced both CA1 (P < 0.001) and CA3 (P < 0.01) neuronal density compared to controls. Minocycline treatment partially reversed the above neurobehavioral and biochemical changes and improved hippocampal neuronal density in MetS animals.
CONCLUSION: MetS led to hippocampal oxidative stress and neuroinflammatory changes with a corresponding loss of hippocampal neuronal density and cognitive decline. Anti-inflammatory and antioxidant property of minocycline may be responsible for its neuroprotective actions in these animals.
The present study deals with the development of hydroxyapatite (HAp)-ciprofloxacin bone-implants using the »Quality by design« approach. The effect of various synthesis parameters like drug amount ...added in the process, stirring speed and addition rate of orthophosphoric acid in the synthesis on drug concentration in the HAp-ciprofloxacin system synthesized by the precipitation technique using 23 factorial design was analyzed. Optimization methodology utillizing the first-order polynomial equation was used to search for optimal drug concentration in the HAp-ciprofloxacin implant system. The observed responses coincided well with the predicted values from the optimization technique. New implants were manufactured using various HAp-ciprofloxacin composites and 1.5 % (m/V) guar gum as a binder. Characterization of the delivery system was done by XRPD, FTIR spectroscopy and SEM. Even at highest drug concentration (76.6 ± 0.5 %, m/m), ciprofloxacin was present in noncrystalline state. The in vitro ciprofloxacin release from various bone-implants was sustained for several weeks and the drug release pattern correlated well with the Korsmeyer- Peppas model.
U radu je opisan razvoj hidroksiapatit (HAp)-ciprofloksacin implantata za kosti »dizajniranjem kvalitete«. Učinak nezavisnih varijabli poput količine dodanog lijeka, brzine miješanja i udjela ortofosforne kiseline na koncentraciju lijeka u HAp-sustavu dobivenom precipitacijom optimiran je koristeći 23 faktorijalno dizajniranje. Pomoću polinomske jednadžbe prvog reda određena je optimalna koncentracija lijeka u implantatima na bazi HAp. Dobiveni odgovori podudaraju se s predviđenim vrijednostima iz optimiranih formulacija. Novi implantati pripravljeni su koristeći različite omjere HAp i ciprofloksacina te 1,5 % (m/V) guar gumu kao vezivo. Karakterizacija sustava za isporuku provedena je pomoću XRPD, FTIR spektroskopije i SEM. Ciprofloksacin je prisutan u amorfnom stanju čak pri najvišim koncentracijama (76,6 ± 0,5 %, m/m). In vitro oslobađanje ciprofloksacina iz različitih implantata bilo je polagano tijekom nekoliko tjedana i dobro je koreliralo s Korsmeyer-Peppasovim modelom.
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Vascular Endothelial Growth Factor (VEGF) has a greater impact on carcinogenesis, and it is the most significant receptor in mediating the mutagenesis and permeability of endothelial ...cells. Here, we report the identification of potential VEGFR-2 inhibitors as new putative anti-cancer agents. In this regard, a pharmacophore model was generated, considering established potent VEGFR2 inhibitors. This model was further applied for the virtual screening of the ZINC database and the feature-based design of another eight molecules (B1–B8). Examining these molecules using sequential computational approaches including molecular docking, molecular dynamic simulation, and DFT analysis leads to the identification of compounds B3, B5, and B7 as potential inhibitors that showed better binding affinity, stability, and interaction mechanisms concerning the reference control, Sorafenib. Further, the Lipinski rule filters and ADMET analysis support the selected compounds as drug candidates subjected to experimental validation.
The present study deals with the development of transferosomal gel containing insulin by reverse phase evaporation method for painless insulin delivery for use in the treatment of insulin dependent ...diabetes mellitus. The effect of independent process variables like ratio of lipids (soya lecithin:cholesterol), ratio of lipids and surfactants, and ratio of surfactants (Tween 80:sodium deoxycholate) on the in vitro permeation flux (μg/cm2/h) of formulated transferosomal gels containing insulin through porcine ear skin was optimized using 23 factorial design. The optimal permeation flux was achieved as 13.50±0.22μg/cm2/h with drug entrapment efficiency of 56.55±0.37% and average vesicle diameter range, 625–815nm. The in vitro insulin permeation through porcine ear skin from these transferosomal gel followed zero-order kinetics (R2=0.9232–0.9989) over a period of 24h with case-II transport mechanism. The in vitro skin permeation of insulin from optimized transferosomal gel by iontophoretic influence (with 0.5mA/cm2 current supply) also provided further enhancement of permeation flux to 17.60±0.03μg/cm2/h. The in vivo study of optimized transferosomal gel in alloxan-induced diabetic rat has demonstrated prolonged hypoglycemic effect in diabetic rats over 24h after transdermal administration.
The goal of any novel drug delivery system is to provide therapeutic benefits to the patients by increasing duration of drug action, reducing dosing frequency, and controlling drug release rate at ...the target site, thereby reducing unwanted side effects. Advanced Technology for Delivering Therapeutics is a reference book that covers recent developments in the field of drug delivery science and technology. The purpose of this book is to bring together descriptions of some selective technologies including new and promising nanotechnology currently being investigated for drug delivery applications. This book is a useful source of information for graduate and post-graduate students of pharmacy and biomedical science; pharmaceutical & other researchers involved in designing newer drug delivery systems both in academia and industry.
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