Abstract
Purpose: To characterize diclofenac sodium (DS) liposomes prepared using palm oil fractions.Methods: Reverse-phase evaporation method was used to prepare liposomes containing 10, 20, 30 , 40 or 50% palm oil fractions. The effect of palm oil content on liposome formation, surface morphology, shape, size and zeta potential of the liposomes were studied using scanning electron microscopy (SEM) transmission electron microscopy (TEM) and particle analyzer. Drug loading, entrapment efficiency and in vitro drug release were measured in phosphate-buffered saline (PBS, pH 7.4) by UV spectrophotometry.Results: TEM and SEM images showed formation of liposomes for all formulations, However, increase in the proportion of palm oil in the formulations significantly reduced particle size and increased zeta potential. The effect on drug loading and drug release varied with palm oil fraction. The best release pattern with appropriate entrapment efficiency and stability was obtained with liposomes containing 33 % palm oil fraction. Introduction of 46 and 56 % of palm oil fractions yielded zeta potential of -42.8 and - 50.7 mV, respectively, compared with -31.2 mV for the formulation without palm oil.Conclusion: The results demonstrate the potentials of palm oil fractions in the preparation of suitable DS liposomes with good bioavailability.Keywords: Liposome, Drug delivery, Palm oil, Diclofenac.
Highlights
Liposome is uni- or multi-layered spherical vesicles mainly composed of phospholipids [1]
The results demonstrate the potentials of palm oil fractions in the preparation of suitable Diclofenac sodium (DS) liposomes with good bioavailability
The main objectives of this study was to investigate the effect of palm oil fraction on formation of liposomes, to assess the stability of liposomal DS prepared by palm oil fraction, to investigate the in vitro drug release rate from new formulation of liposomal DS and to make recommendation based on the best formulation of liposomal DS prepared by palm oil fraction as a parentral drug delivery system
Summary
Liposome is uni- or multi-layered spherical vesicles mainly composed of phospholipids [1]. They are used to deliver both hydrophilic and hydrophobic drugs by various routes of administration such as oral, intramuscular, intraperitoneal, subcutaneous, inhalation and ocular routes [2]. Liposomal encapsulation of drugs can provide targeted drug delivery and sustained release effect besides reduction of toxicity and adverse effects [3]. Available DS dosage forms include gel, ophthalmic solution, immediate and controlled release tablets, suppositories and intramuscular injection [4]. Oral forms of DS are the most common in the market though they usually cause gastrointestinal problems such as abdominal cramps, nausea, constipation, diarrhea and peptic ulceration. Due to its poor solubility in water and acidic medium in the stomach, it has a poor oral bioavailability and a short half-life of about two hours [5]
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