Levofloxacin loaded chitosan and poly-lactic-co-glycolic acid nano-particles against resistant bacteria: Synthesis, characterization and antibacterial activity.

With the global increase in antibacterial resistance, the challenge faced by developing countries is to utilize the available antibiotics, alone or in combination, against resistant bacterial strains. We aimed to encapsulate the levofloxacin (LVX) into polymeric nanoparticles using biodegradable polymers i.e. Chitosan and PLGA, estimating their physicochemical characteristics followed by functional assessment as nanocarriers of levofloxacin against the different resistant strains of bacteria isolated from biological samples collected from tertiary care hospital in Lahore, Pakistan. LVX-NPs were synthesized using ion gelation and double emulsion solvent-evaporation method employing chitosan (CS) and poly-lactic-co-glycolic acid (PLGA), characterized via FTIR, XRD, SEM, and invitro drug release studies, while antibacterial activity was assessed using Kirby-Bauer disc-diffusion method. Data revealed that the levofloxacin-loaded chitosan nanoparticles showed entrapment efficiency of 57.14% ± 0.03 (CS-I), 77.30% ± 0.08(CS-II) and 87.47% ± 0.08 (CS-III). The drug content, particle size, and polydispersity index of CS-I were 52.22% ± 0.2, 559 nm ± 31 nm, and 0.030, respectively, whereas it was 66.86% ± 0.17, 595 nm ± 52.3 nm and 0.057, respectively for CS-II and 82.65% ± 0.36, 758 nm ± 24 nm and 0.1, respectively for CS-III. The PLGA-levofloxacin nanoparticles showed an entrapment efficiency of 42.80% ± 0.4 (PLGA I) and 23.80% ± 0.4 (PLGA II). The drug content, particle size and polydispersity index of PLGA-I were 86% ± 0.21, 92 nm ± 10 nm, and 0.058, respectively, whereas it was 52.41% ± 0.45, 313 nm ± 32 nm and 0.076, respectively for PLGA-II. The XRD patterns of both polymeric nanoparticles showed an amorphous nature. SEM analysis reflects the circular-shaped agglomerated nanoparticles with PLGA polymer and dense spherical nanoparticles with chitosan polymer. The in-vitro release profile of PLGA-I nanoparticles showed a sustained release of 82% in 120 h and it was 58.40% for CS-III. Both types of polymeric nanoparticles were found to be stable for up to 6 months without losing any major drug content. Among the selected formulations, CS-III and PLGA-I, CS-III had better antibacterial potency against gram+ve and gram-ve bacteria, except for K. pneumonia, yet, PLGA-I demonstrated efficacy against K. pneumonia as per CSLI guidelines. All formulations did not exhibit any signs of hemotoxicity, nonetheless, the CS-NPs tend to bind on the surface of RBCs. These data suggested that available antibiotics can effectively be utilized as nano-antibiotics against resistant bacterial strains, causing severe infections, for improved antibiotic sensitivity without compromising patient safety.

Hayee R ，Iqtedar M ，Albekairi NA ，Alshammari A ，Makhdoom MA ，Islam M ，Ahmed N ，Rasool MF ，Li C ，Saeed H ... -  《-》

Preparation and characterization of surface-modified PLGA-polymeric nanoparticles used to target treatment of intestinal cancer.

Ahmad N ，Alam MA ，Ahmad R ，Naqvi AA ，Ahmad FJ ... -  《-》

Enhanced Anti-Proliferative Effect of Carboplatin in Ovarian Cancer Cells Exploiting Chitosan-Poly (Lactic Glycolic Acid) Nanoparticles.

The present article aimed to enhance the therapeutic efficacy of carboplatin (CP) using the formulation of chitosan-poly (lactic glycolic acid) nanoparticles (CS-PLGA NPs). Nanoparticles were synthesized by an ionic gelation method and were characterized for their morphology, particle size, and surface potential measurements by TEM and zeta sizer. This study was highlighted for the evaluation of drug entrapment, loading and in vitro drug release capabilities of the prepared nanoparticles by spectrophotometric analysis. The stability study was also conducted after 3 months for their particle size, zeta potential, drug loading and encapsulation efficiencies. Further, ovarian cancer cell line PEO1 was used to evaluate the toxicity and efficacy of nano-formulation by MTT assay. Additionally, the study was evaluated for apoptosis using flow cytometric analysis. The CS-PLGA-CP NPs were uniform and spherical in shape. The particle size and zeta potential of CS-PLGA-CP NPs were measured to be 156 ±6.8 nm and +52 ±2.4 mV, respectively. High encapsulation (87.4 ± 4.5%) and controlled retention capacities confirmed the efficiency of the prepared nanoparticles in a time and dose-dependent manner. The cytotoxicity assay results also showed that CS-PLGA-CP NPs have a high efficiency on PEO1 cells compared to the free drug. The flow cytometric result showed 64.25% of the PEO1 cells were apoptotic, and 8.42% were necrotic when treated with CS-PLGA-CP NPs. Chitosan-PLGA combinational polymeric nanoparticles were not only steady but also non-toxic. Our experiments revealed that the chitosan-PLGA nanoparticles could be used as a challenging vehicle candidate for drug delivery for the therapeutic treatment of ovarian cancer.

Alassaif FR ，Alassaif ER ，Kaushik AK ，Dhanapal J ... -  《-》

Improved mucoadhesion and cell uptake of chitosan and chitosan oligosaccharide surface-modified polymer nanoparticles for mucosal delivery of proteins.

Dyawanapelly S ，Koli U ，Dharamdasani V ，Jain R ，Dandekar P ... -  《-》

Controlled synthesis of in-situ gold nanoparticles onto chitosan functionalized PLGA nanoparticles for oral insulin delivery.

Chitosan-based nanoparticles (chitosan nanoparticles (ChNps), chitosan gold Nps (ChAuNps), and chitosan gold Nps functionalized with poly lactic-co-glycolic acid (PLGA) (ChAuNps/PLGA)) were prepared as nanocarriers for insulin to improve its oral uptake. The emulsion solvent diffusion method was employed to functionalize the Nps with PLGA. TEM, SEM, DLS, and zeta potential were conducted to characterize the Nps. The morphological analysis confirmed the formation of spherical Nps with hydrodynamic particle sizes of 138±23, 16±2.2, and 50±9.3 nm for ChNps, ChAuNps, and ChAuNps/PLGA, respectively. Zeta potential measurements indicated two types of Nps, regardless of insulin entrapment, positively charged, (ChNps (+36 ± 4.2, +31 ± 2.2mv)) and ChAuNps (+37 ± 4.3, +33 ± 2.5mv) and negatively charged (ChAuNps/PLGA (-31 ± 2.7, -26 ± 2.1 mv)). The in vitro studies were assessed by measuring the entrapment efficiencies (EE%) and the release profiles of insulin at different pH values. EE% for ChNps, ChAuNps, and ChAuNps/PLGA were 97 ± 1.5, 98.4 ± 1.9, and 99 ± 1.2%, respectively. At an acidic medium, a significant level of insulin retention was observed (96 ± 0.08%) for ChAuNps/PLGA. While a high amount was released at higher pH values over an extended period of time. In vivo studies, diabetic rats treated with insulin-loaded Nps had reduced blood glucose level (BGL) (38 ± 2.8, 35 ± 6.5, and 27 ± 5.6%) for ChNps ChAuNps and ChAuNps/PLGA, respectively. The pharmacological availability (PA%) and bioavailability (FR%) for insulin-loaded ChAuNps/PLGA were 15.8 ± 0.71% and 7.7 ± 0.93%, respectively. Altogether, emphasize the role of biocompatible Nps and their efficiency in the convenient delivery of insulin, thus lowering the BGL in a safe condition.

Asal HA ，Shoueir KR ，El-Hagrasy MA ，Toson EA ... -  《-》