Investigation of PEGylated Derivatives of Rosin as Sustained Release Film Formers

Abstract

Abstract. The purpose of the present study was to investigate the potential use of two PEGylated derivatives of rosin (PD) as sustained release film forming materials. The derivatives differed chemically by their acid numbers-PD-1 with 120.93 and PD-2 with 88.19. The derivative films were characterized for surface morphology, water uptake-weight loss, angle of contact, water vapor transmission rate, mechanical properties and permeability study. Dissolution of diclofenac sodium (DS) and propranolol hydrochloride (PHL) as model drugs was studied from coated pellets. The films of derivatives with and without plasticizers were smooth and continuous. PD-2 films developed greater numbers of pores when in contact with phosphate buffer pH 6.8. The low weight loss, low angles of contact and high water vapor transmission rate of PD-2 films were related to presence of higher concentration of PEG esters. Higher tensile strength and percent elongation of PD-2 films was due to greater degree of internal plasticization of the derivative. The permeability of films to model drugs propranolol hydrochloride and diclofenac sodium was inversely proportional to the film thickness and dibutyl phthalate concentration in them; the permeability being greatest in PD-2 films containing 10% PEG 200. Dissolution rate of propranolol hydrochloride was higher from the coated pellets. The dissolution data followed zero order, Baker-Lonsdale equation and Hixon-Crowell equation of release kinetics with high correlation coefficients. The mechanism of drug release from these coated systems however followed class II transport (n>1.0). The derivatives investigated could successfully retard release of the model drugs and offers an alternative to the conventionally used polymers.

Rosin: Recent advances and potential applications in novel drug delivery system

“…43 These rosin microparticulate drug delivery systems provide opportunity not only to be used for controlled drug delivery but also the drug release can be prolonged by increasing the circulation time through PEGylation of rosin microparticles. 44,45 Morkhade et al 46 prepared PEGylated rosin derivatives successfully investigated for their drug loading and release potentials using diclofenac and diltiazem as model drug. PEGylation of rosin and its derivatives can be used to improve the in vivo performance of numerous therapeutic substances such as proteins, peptides and some drug delivery devices such as nanoparticles and microparticles.…”

Study of biodegradation and biocompatibility of PEGylated rosin derivatives

“…PRDs could be used successfully to prepare matrix tablets, coated pellets, and microparticles for sustained drug release. 4,9–11…”

“…PRDs could be used successfully to prepare matrix tablets, coated pellets, and microparticles for sustained drug release. 4,[9][10][11] Simultaneously, with the evaluation of rosin and its polyhydric alcohol-based derivatives for drug delivery applications, attempts were also made to assess their biodegradation and biocompatibility. [12][13][14][15] It was found that the biodegradation and biocompatibility of native rosin and its polyhydric alcohol-based derivatives were comparable to that of poly(d,l-lactide-co-glycolide) (PLGA).…”

Synthesis and Characterization of Water Soluble Rosin-Polyethylene Glycol 1500 Derivative

“…They are monocarboxylic acids of alkylated hydrophenanthrene; abietic acid constitutes the principal resin acid. [3], [4]. It is soluble in alcohol, ether, benzene and chloroform but insoluble in water Polyethylene glycol (PEG) or poly (ethylene oxide) is petroleum base polymer represent water-soluble mono hydroxy alcohols.…”