ABSTRACT
OBJECTIVE: The efficient inhibition of bacteria and their by-products from infected root canals is hampered by the limitations of traditional root canal disinfection strategies, bacterial resistance to antibiotic drugs, and regenerative endodontics. Polymeric nanoparticles nanocarrier for controlling antibiotic drug delivery were used to overcome the limitations encountered in endodontics treatment. BACKGROUND: Several polymeric nanoparticles have been used for the delivery of ciprofloxacin drug. The application of poly (ethylene glycol) methyl ether-block-poly(lactide-co-glycolide) (PEG-PLGA) nanoparticles has highlighted the clean and safe delivery of ciprofloxacin (CIP) hydrophilic drug for endodontics treatment. PEG/PLGA was prepared using the solid/oil/water method and the CIP was loaded into polymeric nanoparticles via an ion pairing agent. RESULTS: The CIP-loaded PEG-PLGA nanoparticles have a spherical shape with a 120 ± 0.43 nm size, the CIP encapsulating efficiency was 63.26 ± 9.24% with a loading content of 7.75 ± 1.13%, and sustained release was achieved over 168 h which followed Higuchi model with a non-Fickian mechanism. Moreover, CIP-loaded PEG-PLGA had low cytotoxicity to the stem cells of the apical papilla. CONCLUSION: The results conclude invigorating future perspectives of polymeric nanoparticles for a wide range of drug delivery for various disease treatments. It's anticipated that these polymeric nanoparticles may divert new expectations in the future for topical antibiotic drug delivery with discrete intracellular medicament, and a safe and clean environment.
Subject(s)
Anti-Bacterial Agents , Ciprofloxacin , Drug Resistance, Bacterial , Nanoparticles , Polyethylene Glycols , Ciprofloxacin/pharmacology , Ciprofloxacin/administration & dosage , Ciprofloxacin/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/administration & dosage , Anti-Bacterial Agents/chemistry , Polyethylene Glycols/chemistry , Nanoparticles/chemistry , Drug Carriers/chemistry , Humans , Drug Liberation , Nanoparticle Drug Delivery System/chemistry , Microbial Sensitivity Tests , Particle Size , Cell Survival/drug effects , PolyestersABSTRACT
(-)-Colchicine, an anti-microtubulin polymerization agent, is a valuable medication and the drug of choice for gout, Behçet's disease and familial Mediterranean fever. It has a narrow therapeutic index due to its high toxicity towards normal cells. Nonetheless, numerous (-)-colchicine derivatives have been synthesized and studied for their structure-activity relationship and preferential toxicity. Different functional groups such as amides, thioamides, N-arylurea and 8,12-diene cyclic have been incorporated into (-)-colchicine, resulting in derivatives (with moieties) that include electron-withdrawing and electron-donating groups. This review article focuses on recent developments in the chemical synthesis of (-)-colchicine derivatives, the substituents used, the functional groups linked to the substituents, the moieties and biological studies. Moreover, the current classification of derivatives based on the (-)-colchicine rings, namely ring A, B, and C (-)-colchicine derivatives, is discussed. This work demonstrates and summarizes the significance of (-)-colchicine derivatives in the biological field, and discusses their promising therapeutics for the future.
Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Colchicine/pharmacology , Neoplasms/drug therapy , Antineoplastic Agents, Phytogenic/chemical synthesis , Antineoplastic Agents, Phytogenic/chemistry , Cell Proliferation/drug effects , Colchicine/analogs & derivatives , Colchicine/chemical synthesis , Colchicine/chemistry , Humans , Molecular Structure , Neoplasms/pathologyABSTRACT
Antimitotic colchicine possesses low therapeutic index due to high toxicity effects in non-target cell. However, diverse colchicine analogs have been derivatized as intentions for toxicity reduction and structure-activity relationship (SAR) studying. Hybrid system of colchicine structure with nontoxic biofunctional compounds modified further affords a new entity in chemical structure with enhanced activity and selectivity. Moreover, nanocarrier formulation strategies have been used for colchicine delivery. This review paper focuses on colchicine nanoformulation, chemical synthesis of colchicine prodrugs and codrugs with different linkers, highlights linker chemical nature and biological activity of synthesized compounds. Additionally, classification of colchicine prodrugs based on type of conjugates is discussed, as biopolymers prodrugs, fluorescent prodrug, metal complexes prodrug, metal-labile prodrug and bioconjugate prodrug. Finally, we briefly summarized the biological importance of colchicine nanoformulation, colchicine prodrugs and codrugs.
