Fabrication and in vitro evaluation of chitosan-gelatin based aceclofenac loaded scaffold.

Scaffold development is a nascent field in drug development. The scaffolds mimic the innate microenvironment of the body. The goal of this study was to formulate a biocompatible and biodegradable scaffold, loaded with an analgesic drug, aceclofenac (Ace). The bioscaffold is aimed to have optimum mechanical strength and rheology, with drug released in a sustained manner. It was prepared via chemical cross-linking method: a chitosan (CS) solution was prepared and loaded with Ace; gelatin (GEL) was added and the mixture was cross-linked to get a hydrogel. 20 formulations were prepared to optimize different parameters including the stirring speed, drug injection rate and crosslinker volume. The optimal formulation was selected based on the viscosity, drug solubility, homogeneity, porosity and swelling index. A very high porosity and swelling index were attained. In vitro release data showed sustained drug delivery, with effective release at physiological and slightly acidic pH. SEM analysis revealed a homogeneous microstructure with highly interconnected pores within an extended polymer matrix. FT-IR spectra confirmed the absence of polymer-drug interactions, XRD provided evidences for efficient drug entrapment within the scaffold. Rheological analysis corroborated the scaffold injectability. Mathematical models were applied to in-vitro data, and the best fit was attained with Korsmeyer-Peppas.

Design and Evaluation of pH Sensitive PEG-Protamine Nanocomplex of Doxorubicin for Treatment of Breast Cancer.

Cancer is the most common cause of mortality worldwide. There is dire need of modern strategies-such as surface modification of nanocarriers-to combat this global illness. Incorporation of active targeting ligands has arisen as a novel platform for specific tumor targeting. The aim of the current study was to formulate PEG-protamine complex (PPC) of doxorubicin (DOX) for treatment of breast cancer (BC). DOX coupling with PEG can enhance cell-penetrating ability: combating resistance in MDA-MB 231 breast cancer cells. Ionic gelation method was adopted to fabricate a pH sensitive nanocomplex. The optimized nanoformulation was characterized for its particle diameter, zeta potential, surface morphology, entrapment efficiency, crystallinity, and molecular interaction. In vitro assay was executed to gauge the release potential of nanoformulation. The mean particle size, zeta potential, and polydispersity index (PDI) of the optimized nanoparticles were observed to be 212 nm, 15.2 mV, and 0.264, respectively. Crystallinity studies and Fourier transform infrared (FTIR) analysis revealed no molecular interaction and confirmed the amorphous nature of drug within nanoparticles. The in vitro release data indicate sustained drug release at pH 4.8, which is intracellular pH of breast cancer cells, as compared to the drug solution. PPC loaded with doxorubicin can be utilized as an alternative and effective approach for specific targeting of breast cancer.

Proniosomes as a Carrier System for Transdermal Delivery of Clozapine.

The current study aimed to formulate the clozapine (CLZ) loaded proniosomal gel (PN) and evaluate it's in vitro release, ex vivo permeation and gel properties. CLZ is a BCS class II drug with low bioavailability of 27% and severe adverse drug reactions (ADRs) due to frequent dosing. Proniosomes offer a versatile pro-vesicular approach with potential in transdermal drug delivery. PN-CLZ gel was prepared by the coacervation phase separation method utilizing span-60, cholesterol and lecithin. Optimization of PN gel was done by hit & trial method and the formulations were characterized for particle size, entrapment efficiency (EE), polydispersity index (PDI) and zeta potential (ZP). The optimized formulation had the highest entrapment efficiency of 90% and the average particle size of approx. 325 nm. PDI reflected homogeneity in the formulation. ZP was -59.76 mV, high enough to indicate a stable formulation. The in vitro release studies manifested a sustained release behavior of clozapine from the proniosomal gel. The ex vivo permeation showed noteworthy permeation of the drug through stratum corneum with a steady state flux of 18.26 ug/cm2/hr. The optimized gel was analyzed for pH, spreadability, bioadhesion and rheology. The results suggested that clozapine could be effectively loaded into proniosomal gel for administration through skin.