Microencapsulation of protein into biodegradable matrix: a smart solution cross-linking technique.

Sustained-release albumin microspheres (MSs) can be obtained by chemically cross-linking albumin. However, a significant challenge is preventing the cross-linking of the active pharmaceutical (protein or small molecule) ingredient (API) with the MS matrix. To prevent cross-linking of the API with the albumin matrix, a smart "solution cross-linking-microencapsulation" method was developed which involves cross-linking albumin solution with glutaraldehyde first, neutralizing any excess glutaraldehyde with sodium bisulphite, followed by the addition of API and finally spray drying.

Formulation and in vitro characterization of spray-dried antisense oligonucleotide to NF-kappaB encapsulated albumin microspheres.

The aim of this study was to formulate and characterize microspheres containing antisense oligonucleotide to NF-kappaB using bovine serum albumin as the polymer matrix. Microspheres were prepared by spray-drying technique with 5, 10 and 15% drug loading. Glutaraldehyde was used as a cross-linking agent.

Oral delivery of gastro-resistant microencapsulated typhoid vaccine.

Oral vaccination has long been regarded as the best alternative to conventional parenteral vaccination considering practical, economical, and immunological aspects. The purpose of this study was to develop albumin-chitosan mixed matrix microsphere-filled coated capsule formulations of Typhoid Vi antigen and to determine whether it can induce antigen-specific mucosal and systemic immune responses on oral administration. Formulations with Typhoid Vi antigen were prepared and filled into hard gelatin capsules (size # 9) and enteric coated.

A methodology for quantitation and characterization of oligonucleotides in albumin microspheres.

A fluorescence assay was developed to quantify oligonucleotides (ODNs) encapsulated in bovine serum albumin (BSA) microspheres using antisense to Nuclear Factor-kappaB (NF-kappaB) as a model ODN and employing Oligreen as the fluorescent dye. Methodologies were optimized for the suspension of the microspheres as well as release of the encapsulated ODN using protease digestion. This was followed by the detection and quantitation of the ODN using the Oligreen dye.

Formulation and evaluation of albumin microspheres and its enteric coating using a spray-dryer.

This study optimized and evaluated the conditions for surface coating of microspheres using a spray-dryer. Four formulations of Bromophenol blue (BPB)-loaded albumin microspheres were prepared using a spray-dryer, cross-linked at different concentrations and time periods. One of the optimized formulations with the desired characteristics was selected for enteric coating with Eudragit L100-55.

Oral delivery of low molecular weight heparin microspheres prepared using biodegradable polymer matrix system.

Parenteral route is preferred for low molecular weight heparin (LMWH) due to poor oral bioavailability. Biodegradable formulation components were evaluated for possible interactions between the physical mixtures using differential scanning calorimetry. LMWH and an absorption enhancer papain were encapsulated in bovine serum albumin matrix and four formulations were spray-dried (MS.

Treatment of adjuvant arthritis using microencapsulated antisense NF-κB oligonucleotides.

Antisense oligonucleotides are promising new therapeutic agents used to selectively inhibit target genes such as Nuclear Factor Kappa B (NF-κB), an important transcription factor in the pathogenesis of inflammatory disease. The purpose of the present study was to evaluate microencapsulated antisense oligonucleotides specific to NF-κB for in vitro efficacy and treatment of adjuvant-induced arthritis in rats. Oligonucleotide-loaded albumin microspheres were prepared and characterized in terms of size, zeta potential, morphology and release pattern.