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Natural polymer guar gum has one of the highest viscosities in water solution and hence, these are significantly used in pharmaceutical applications. Guar gum inter-connected micelles as a new carrier has been developed for poor water soluble rifampicin drug. The hydrogel inter-connected micelle core was formulated as a hydrophilic inner and hydrophobic outer core by using guar gum/chitosan/polycaprolactone and the carrier interaction with rifampicin was confirmed by FT-IR. The morphological observations were carried out through TEM, SEM and AFM analysis. The encapsulation efficiency and in-vitro drug release behavior of prepared hydrogel based micelle system was analyzed by UV–vis spectrometry. The anti-bacterial activity against K. pneumoniae and S. aureus was studied by observing their ruptured surface by SEM. The cytotoxicity study reveals that the pure polymeric system has no toxic effect whereas drug loaded ones showed superior activity against THP-1 cells. From the cell apoptosis analyses, the apoptosis was carried out in a time dependent manner. The cell uptake behavior was also observed in THP-1 cells which indicate that the hydrogel based micelle system is an excellent material for the mucoadhesive on intracellular alveolar macrophage treatment.

This study demonstrates the development of pH and thermosresponsive nanoparticles (NPs) composed via cholic acid, PCPP-PLA hybrid polymer integrated with indocyanine green (ICG) for site specific delivery hydrophobic drug (paclitaxel). Drug and ICG were physically encapsulated by poly (bis(carboxyphenoxy)phosphazene) (PCPP)-poly lactic acid hybrid polymer. The hybrid polymer solution showed reversible gelation behaviour at the temperature between 37 °C and 20 °C and also it showed pH dependent drug release capability at acidic pH due to the pH responsive quenching effects of PCPP-PLA. The size (150–200 nm) and morphology of drug-loaded polymeric NPs were characterized using SEM and HR-TEM. Further, the release of loaded paclitaxel (PTX) from polymer was significantly sustained over 12 days. Drug release from the nanoparticles was effectively controlled by the mechanical strength of the polymer. All of these results demonstrate that pH triggered hybrid polymeric NPs are potential carriers for tumor-targeted drug delivery and also it exhibits great strength at 37 °C.

Our aim was to evaluate the capacity of polymeric nanoparticles (PNPs) to selectively deliver an antituberculosis drug (rifampicin; RF) to alveolar macrophages. Anionic biodegradable copolymer sodium alginate-g-allylamine-mannose (SA-g-AA-M) was synthesized by atom transfer free radical polymerization and direct coupling of the respective conjugates. The fabrication of RF-loaded Zn2+ ion-cross-linked SA-g-AA-M PNPs was conducted by an O/W emulsion method followed by ionotropic gelation. The structural nature of the RF-loaded SA-g-AA-M PNPs was analyzed by Fourier transform infrared (FT-IR) spectroscopy. Meanwhile, scanning electron microscopy (SEM) and transmission electron microscopy (TEM) were used to illustrate the shape and morphology of the nanoparticles. The PNPs were observed as uniform spheres in the nanometer range (

We have developed a nano drug delivery system for the treatment of tuberculosis (TB) using rifampicin (RF) encapsulated in poly(ester amide)s nanoparticles (PEA-RF-NPs), which are biocompatible polymers. In this study, biodegradable amino acid based poly(ester amide)s (PEAs) were synthesized by the poly condensation reaction and RF-loaded NPs were fabricated by the dialysis method. The surface morphology and in-vitro drug release efficiency were examined. The effect of time and temperature on the cellular uptake of PEA-RF-NPs in NR8383 cells was evaluated. Fluorescence microscopic results of PEA-RF-NPs from NR8383 cell lines suggest its potential application in treating TB. The antibacterial activity of RF against Mycobacterium smegmatis was also evaluated. Based on these results, this approach provides a new means for controlled and efficient release of RF using the PEA-NPs delivery system and is promising for the treatment of TB. M. Rajan is grateful to the DST-SERB, Government of India, for financial support under the scheme of �EMEQ� (F.No.- SB/EMEQ-241-2014) and University Grants Commission UGC-MRP scheme Ref: No. F.43-187/2014 (SR), New Delhi. The authors would like to extend their sincere appreciation to the Deanship of Scientific Research at King Saud University for its funding of this research through Research Group project No. RG-1435-057. M. Rajan thanks the DST-FIST program for the purchase of an FTIR, SEM, and the UGC, for funds under UPE programs for the purchase of a TEM. Scopus

The physiological environment is a crucial factor in biomedical systems, which can be regulated with relative ease both in vitro and in vivo. Control of pH has emerged as a powerful strategy in cancer therapy because pH has a profound effect on the interaction of a polymeric-based drug delivery system with tumor cells. In this regard, the enhancement of pH response capability was demonstrated with a 5-flourouracil (5-FU)-loaded guar gum (GG)-grafted-lysine-?-cyclodextrin (L-?-CD) drug carrier. The size, charge, morphology, and encapsulation efficiency of the 5-FU-loaded polymeric carrier were characterized for the control and sustained release of the drug. In a specific cancer pH environment, 5-FU-loaded GG-g-L-?-CD could rapidly swallow, disassemble, and release 5-FU by accepting or losing electrons. In vitro observations indicate that GG-g-L-?-CD dramatically releases 5-FU in an acidic environment rather than in a basic environment. In vitro antitumor activity tests showed that 5-FU-loaded GG-g-L-?-CD had a higher cytotoxicity against KB cells, with an IC50 value of 1.38 ?g ml-1. The reactive oxygen species (ROS) generated by 5-FU in the KB cells showed efficient suppression of tumour cell growth. The Hoechst assay revealed the active nature of 5-FU in the cell nucleus of the KB cells. The potential mitochondrial damage by apoptosis in KB cells greatly increased cell death. Therefore, due to its active nature, the pH-sensitive 5-FU-loaded GG-g-L-?-CD carrier is a potential drug delivery system for safe and effective cancer therapy, and it can be useful for inhibiting tumour cell growth. MR acknowledges the major financial support received from the University Grants Commission (UGC), Government of India, for financial support under the plan of ‘‘UGC-MRP’’ (F. No. 43-187/ 2014) (SR) and Department of Science and Technology, Science and Engineering Research Board (Ref: YSS/2015/001532; New Delhi, India), ‘‘EMEQ’’ (F. No. – SB/EMEQ-241-2014) and also acknowledges the PURSE program for the purchase of SEM and FT-IR and UPE programs for the purchase of TEM. Scopus

Amphiphilic chitosan-graft-poly(caprolactone)/(ferulic acid) (CS-g-PCL/FA) multi-co-polymers were fabricated by microwave-assisted ring opening polymerization followed by an 1-ethyl-3-(3-dimethyl-aminopropyl) carbodiimide (EDC)-mediated coupling reaction and characterized by Fourier transformed infrared (FTIR) spectroscopy. Graft copolymers self-assembled into nanomicelles, and were able to incorporate rifampicin (RF) into their hydrophobic inner cores. X-ray diffraction (XRD) patterns were applied to characterize the crystal structures of graft polymers and the effects of RF on micelle morphology. Empty and RF-loaded CS-g-PCL/FA nanomicelles underwent swelling and degradation in acidic pH conditions. Scanning electron microscopy, transmission electron microscopy, and dynamic light scattering revealed that the self-assembled, RF-loaded micelles were spherical, with an average size of 100–210 nm. An in vitro study conducted at 37 °C demonstrated that RF and FA release from micelles at pH 5.3 was much faster than that at pH 7.4. The RF and FA release was significantly accelerated by switching to an acidic pH, owing to swelling of the micelles at lower pH values caused by the rapid degradation of ester and amide bonds present in the micelles. Fluorescence micrographs revealed successful entry of the polymeric micelles into A549cell lines. Thus, graft polymeric micelles have promising potential for delivery of hydrophobic antitubercular drugs and may improve therapeutic approaches for tuberculosis.

Lignin (LIG), one of the major natural polymers in the biomass is widely used for various industrial and biomedical applications, mainly in its modified form of grafted lignin. The present study focuses on the isolation of lignin from Aloe barbadensis Miller by a microwave extraction technique and its applicability as a medicinal biomass. The isolated lignin was used for the synthesis of a drug carrier by grafting with methacrylate (MA). Lignin grafted methacrylate was synthesised (LIG-g-MA) via atom transfer radical polymerization (ATRP). 5-Fluorouracil (5-FU) was used as a model cancer drug and it was encapsulated on the hollow nanocarrier by the emulsion/solvent evaporation technique. While NMR spectroscopy elucidates the structure of the isolated lignin, FT-IR and XRD techniques address the binding nature and crystalline character of 5-FU loaded carrier. The surface morphology of the isolated lignin, grafted lignin and drug-loaded carrier was confirmed with SEM and TEM techniques. The encapsulation efficiency and in vitro drug release were studied to determine the efficiency of the carrier. The cell viability and cytotoxicity effect of 5-FU loaded on LIG-g-MA and unloaded LIG-g-MA were performed against MCF-7 and VERO cell lines. In short, the modified natural lignin based on LIG-g-MA hollow-nanofibrous material has been shown to be a potentially useful biocompatible nanocarrier in chemotherapy for cancer treatment. The Royal Society of Chemistry 2016. Scopus