Development and Evaluation of Novel Self-Nanoemulsifying Drug Delivery Systems Based on a Homolipid from Capra hircus and Its Admixtures with Melon Oil for the Delivery of Indomethacin
In this study, goat fat (Capra hircus) and melon oil were extracted and used to formulate self-nanoemulsifying drug delivery systems (SNEDDS) based on either goat fat alone or its admixture with melon oil by employing escalating ratios of oil(s), surfactant blend (1？:？1 Tween 60 and Tween 80), and cosurfactant (Span 85), with or without carbosil, a glidant, for the delivery of indomethacin. The formulations were encapsulated in hard gelatin capsules and then assessed using isotropicity test, aqueous dilution stability and precipitation propensity, absolute drug content, emulsification time, in vitro drug release, and anti-inflammatory activity. The SNEDDS exhibited low precipitation propensity and excellent stability on copious dilution, as well as high drug release in vitro and in vivo. The inhibition produced by the SNEDDS was comparable to that of indomethacin injection (positive control) for much of the 5？h test period, indicating a high degree of bioavailability of the administered SNEDDS. The absolute drug contents and emulsification times fell within narrow limits. This study has shown that a 1？:？1 ratio of melon oil and goat fat could confer favourable properties with respect to drug release and anti-inflammatory activity on SNEDDS for the delivery of indomethacin, thus encouraging further development of the formulations. 1. Introduction The nonsteroidal anti-inflammatory drugs (NSAIDs) have remained the mainstay of the treatment and management of inflammatory disorders. Despite enormous innovations in novel drug delivery systems (NDDS) through alternative routes, oral drug delivery of NSAIDs has been the most common and preferred route of drug administration [1]. Its status is primarily a consequence of the wide acceptability of this “natural” route, better safety vis-à-vis the parenteral route, low cost of therapy, and improved patient compliance. With an increasing number of lipophilic drugs under development, homolipids and heterolipids have gained renewed interests as excipients for myriads of drug delivery systems [2]. Lipid-based formulations have been shown to enhance the bioavailability of orally administered drugs [3–6]. The oral delivery of lipophilic drugs presents a major challenge because of the low aqueous solubility. The Biopharmaceutics classification system (BCS) [7] classifies drugs into four categories depending on their solubility and permeability characteristics. According to this scheme, indomethacin belongs to class II drugs whose solubility is too low to be consistent with complete absorption. For this class of
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