title: RGD-TPGS decorated theranostic liposomes for brain targeted delivery.
abstract: The aim of this work was to formulate RGD-TPGS decorated theranostic liposomes, which contain both docetaxel (DTX) and quantum dots (QDs) for brain cancer imaging and therapy. RGD conjugated TPGS (RGD-TPGS) was synthesized and conjugation was confirmed by Fourier transform infrared (FTIR) spectroscopy and electrospray ionisation (ESI) mass spectroscopy (ESI-MS). The theranostic liposomes were prepared by the solvent injection method and characterized for their particle size, polydispersity, zeta-potential, surface morphology, drug encapsulation efficiency, and in-vitro release study. Biocompatibility and safety of theranostic liposomes were studied by reactive oxygen species (ROS) generation study and histopathology of brain. In-vivo study was performed for determination of brain theranostic effects in comparison with marketed formulation (Docel™) and free QDs. The particle sizes of the non-targeted and targeted theranostic liposomes were found in between 100 and 200nm. About 70% of drug encapsulation efficiency was achieved with liposomes. The drug release from RGD-TPGS decorated liposomes was sustained for more than 72h with 80% of drug release. The in-vivo results demonstrated that RGD-TPGS decorated theranostic liposomes were 6.47- and 6.98-fold more effective than Docel™ after 2h and 4h treatments, respectively. Further, RGD-TPGS decorated theranostic liposomes has reduced ROS generation effectively, and did not show any signs of brain damage or edema in brain histopathology. The results of this study have indicated that RGD-TPGS decorated theranostic liposomes are promising carrier for brain theranostics.
authors: Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, India.
authors: Sonali
authors: Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, India.
authors: Rahul Pratap
authors: RP
authors: Singh
authors: Genotoxicology and Cancer Biology Lab, Department of Zoology, Institute of Science, Banaras Hindu University, Varanasi, 221005, India.
authors: Gunjan
authors: G
authors: Sharma
authors: Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi, 221005, India.
authors: Lakshmi
authors: L
authors: Kumari
authors: Genotoxicology and Cancer Biology Lab, Department of Zoology, Institute of Science, Banaras Hindu University, Varanasi, 221005, India.
authors: Biplob
authors: B
authors: Koch
authors: Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi, 221005, India.
authors: Sanjay
authors: S
authors: Singh
authors: Department of Pathology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, India.
authors: Shreekant
authors: S
authors: Bharti
authors: School of Pharmacy, Taylors University, Kuala Lumpur, 47500, Malaysia.
authors: Paruvathanahalli Siddalingam
authors: PS
authors: Rajinikanth
authors: Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, India.
authors: Bajarangprasad L
authors: BL
authors: Pandey
authors: Department of Pharmaceutics, Indian Institute of Technology (BHU), Varanasi, 221005, India; Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi, 221005, India. Electronic address: muthubits@rediffmail.com.
authors: Madaswamy S
authors: MS
authors: Muthu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000494:pharmacology; D001921:Brain / Q000187:drug effects*; D001932:Brain Neoplasms / Q000188:drug therapy; D000077143:Docetaxel; D004337:Drug Carriers; D016503:Drug Delivery Systems; D065546:Drug Liberation; D008081:Liposomes / Q000737:chemistry*; D053758:Nanoparticles / Q000008:administration & dosage / Q000737:chemistry; D045663:Quantum Dots; D051381:Rats; D011919:Rats, Inbred Strains; D017382:Reactive Oxygen Species / Q000378:metabolism; D043823:Taxoids / Q000008:administration & dosage / Q000494:pharmacology*; D000068936:Theranostic Nanomedicine; D014810:Vitamin E / Q000737:chemistry*
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D008081:Liposomes; D017382:Reactive Oxygen Species; D043823:Taxoids; D014810:Vitamin E; D000077143:Docetaxel; C014225:tocophersolan
keywords: Brain cancer; RGD-TPGS; Safety; Targeted nanomedicine; Theranostic liposomes