title: Enhanced efficacy of clindamycin hydrochloride encapsulated in PLA/PLGA based nanoparticle system for oral delivery.
abstract: Clindamycin hydrochloride (CLH) is a clinically important oral antibiotic with wide spectrum of antimicrobial activity that includes gram-positive aerobes (staphylococci, streptococci etc.), most anaerobic bacteria, Chlamydia and certain protozoa. The current study was focused to develop a stabilised clindamycin encapsulated poly lactic acid (PLA)/poly (D,L-lactide-co-glycolide) (PLGA) nano-formulation with better drug bioavailability at molecular level. Various nanoparticle (NPs) formulations of PLA and PLGA loaded with CLH were prepared by solvent evaporation method varying drug: polymer concentration (1:20, 1:10 and 1:5) and characterised (size, encapsulation efficiency, drug loading, scanning electron microscope, differential scanning calorimetry [DSC] and Fourier transform infrared [FTIR] studies). The ratio 1:10 was found to be optimal for a monodispersed and stable nano formulation for both the polymers. NP formulations demonstrated a significant controlled release profile extended up to 144 h (both CLH-PLA and CLH-PLGA). The thermal behaviour (DSC) studies confirmed the molecular dispersion of the drug within the system. The FTIR studies revealed the intactness as well as unaltered structure of drug. The CLH-PLA NPs showed enhanced antimicrobial activity against two pathogenic bacteria Streptococcus faecalis and Bacillus cereus. The results notably suggest that encapsulation of CLH into PLA/PLGA significantly increases the bioavailability of the drug and due to this enhanced drug activity; it can be widely applied for number of therapies.
authors.affiliation: Immunology and Molecular Medicine Lab, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India.
authors.forename: Pradipta Ranjan
authors.initials: PR
authors.lastname: Rauta
authors.affiliation: Immunology and Molecular Medicine Lab, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India.
authors.forename: Niladri Mohan
authors.initials: NM
authors.lastname: Das
authors.affiliation: Immunology and Molecular Medicine Lab, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India.
authors.forename: Debasis
authors.initials: D
authors.lastname: Nayak
authors.affiliation: Immunology and Molecular Medicine Lab, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India.
authors.forename: Sarbani
authors.initials: S
authors.lastname: Ashe
authors.affiliation: Immunology and Molecular Medicine Lab, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India. nayakb@nitrkl.ac.in.
authors.forename: Bismita
authors.initials: B
authors.lastname: Nayak
mesh_terms: D000284:Administration, Oral; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry; D018407:Bacterial Physiological Phenomena / Q000187:drug effects*; D002470:Cell Survival / Q000187:drug effects; D002981:Clindamycin / Q000008:administration & dosage* / Q000737:chemistry*; D003692:Delayed-Action Preparations / Q000008:administration & dosage* / Q000138:chemical synthesis; D004058:Diffusion; D004357:Drug Synergism; D019344:Lactic Acid / Q000737:chemistry*; D053769:Nanocapsules / Q000737:chemistry*; D011100:Polyglycolic Acid / Q000737:chemistry*; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer
chemical_list: D000900:Anti-Bacterial Agents; D003692:Delayed-Action Preparations; D053769:Nanocapsules; D000077182:Polylactic Acid-Polyglycolic Acid Copolymer; D011100:Polyglycolic Acid; D019344:Lactic Acid; D002981:Clindamycin