Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers

Abstract

Nanostructured lipid carriers (NLCs) have been one of the systems of choice for improving the oral bioavailability of drugs with poor water solubility. In the present study, lovastatin (LVT)-loaded NLCs (LVT-NLCs) were successfully prepared by hot high-pressure homogenization method with high entrapment efficiency, drug loading, and satisfactory particle size distribution. The particles had almost spherical and uniform shapes and were well dispersed with a particle size of <50 nm (23.5±1.6 nm) and a low polydispersity index (0.17±0.05 mV). The result of stability showed that the LVT-NLCs dispersion maintained excellent stability without exhibiting any aggregation, precipitation, or phase separation at 4°C for 6 months of storage. The LVT release data from all developed solid lipid nanoparticles (SLNs) and NLCs were best fitted to a Ritger–Peppas kinetic model (0.9832 and 0.9783 for NLCs and SLNs, respectively). This indicated that the release of LVT from the SLNs and NLCs was due to a combination of drug diffusion and erosion from the lipid matrix. The pharmacokinetic and pharmacodynamic results show that LVT-NLCs were better compared to free drug, which could be attributed to an increase in bioavailability.

Nanomedicine applied to cardiovascular diseases: latest developments

“…It was also shown that LVT-CEN maintains excellent stability without exhibiting any aggregation, precipitation or phase separation after 6 months of storage at 4°C. 21 Additionally, Broz and colleagues have developed a polymeric nanovesicle system for targeted delivery of statins in high doses, thus reducing the toxicity caused by these drugs in other tissues. In this study, the nanovesicles were loaded with pravastatin and their surface was functionalized with an oligonucleotide having high affinity for inflammatory macrophages.…”

Drug Solubility Enhancement through the Preparation of Multicomponent Organic Materials: Eutectics of Lovastatin with Carboxylic Acids

“…Recent studies have shown that LOV can induce tumor cell apoptosis [20], inhibit the mevalonate pathway in breast cancer [21], is considered as a potential drug treatment in gastric cancer [22] and has been trialed in other cancer treatments [23]. Nevertheless, the low bioavailability of LOV related to its poor water solubility [24,25] makes the formulation of this drug for oral administration quite challenging. Several efforts have been made to improve both the solubility and bioavailability of this drug through different approaches, including the synthesis of nanocrystals [26], nanomatrix-supported lipid bilayers [27], microspheres [28], self-nanoemulsifying drug delivery systems [29,30], methylated beta-cyclodextrin [31], solid lipid nanoparticles [32] and nanostructured lipid carriers [25].…”

Inhibition of Zymosan-Induced Inflammatory Factors Expression by ATRA Nanostructured Lipid Carriers

“…NLCs can improve the oral bioavailability of poorly water-soluble drugs. Specifically, NLCs carrying drugs were more effective than the free drugs were because they increased the drug bioavailability [ 31 ]. ATRA is highly lipophilic and poorly soluble in water [ 26 ], and NLCs were able to prolong the release of ATRA [ 32 ].…”