Lipid based nanocarriers: a translational perspective

Phospholipids: Unique carriers for drug delivery systems

Recently, advances in pharmaceutical research is focused on new delivery systems utilizing new devices to achieve modification of delivery time, targeting, as well as improve the in vivo solubility and hence bioavailability of poorly soluble drugs. Lipid based drug delivery systems (LDDS) consists of diverse group of formulations, each consisting of varying functional and structural properties that are amenable to modifications achieved by varying the composition of lipid excipients and other additives. LDDS has evolved, overtime, from micro- to nano-scale enhancing the efficacy and therapeutic application of these systems. LDDS are accepted, proven, commercially viable strategies for formulating challenging pharmaceutical molecules and can be tailored to meet a wide range of product requirements. Generally, most lipid drug delivery systems used as drug carriers have high stability, high carrier capacity, feasibility of incorporating both hydrophilic and hydrophobic substances and feasibility of variable routes of administration, including oral, topical, parenteral and pulmonary routes. LDDS can also be designed to allow modified drug release from matrices. LDDS could be broadly grouped into four: solid lipid particulate dosage forms, emulsion based systems, solid lipid tablets, and vesicular systems. Modifications from these four types include: lipospheres, solid lipid nanoparticles (SLNs), nano structured lipid carriers (NLC), lipid drug conjugate nanoparticles (LDC), self emulsifying formulations (SEFs), pickering emulsions, dry emulsions, micro and nano-emulsions, solidified reverse micellar solution (SRMS) based tablets, liposomes, herbosomes, cryptosomes and transferosomes amongst others. This work exhaustively reviewed the advances in LDDS and also drew comparison between the different types based on history, methods of manufacture, applications, advantages and disadvantages.

	Key words: Cryptosomes, lipospheres, lipoplexes, solid lipid tablets, pharmacosomes, virosomes, vesosomes.

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Lipid-based drug delivery systems (LDDS): Recent advances and applications of lipids in drug delivery

Objective: To formulate sustained-release diclofenac potassium-loaded solid lipid microparticles (SLMs) based on solidified reverse micellar solution (SRMS) and to evaluate the in vitro and in vivo properties.Methods: SRMS consisting of mixtures of Phospholipon® 90H and Softisan® 154 were used to formulate diclofenac potassium-loaded SLMs. Characterization based on the particle size and morphology, stability and encapsulation efficiency (EE%) were carried out on the SLMs. In vitro release was carried out in simulated intestinal fluid (pH 7.5). Anti-inflammatory and ulcerogenic properties were studied using rats.Results: Maximum EE% of 95%, 94% and 93% were obtained for SLMs formulated with SRMS 1:1, 2:1 and 1:2, respectively. In vitro release showed about 85–90% drug release at 13 h. Diclofenac potassium-loaded SLMs showed good anti-inflammatory and gastro-protective properties.Conclusion: Diclofenac potassium-loaded SLMs based on SRMS could be used orally or parenterally under controlled conditions, for ...

Sustained-release diclofenac potassium-loaded solid lipid microparticle based on solidified reverse micellar solution: in vitro and in vivo evaluation

The use of biomaterials composed of organic pristine components has been successfully described in several purposes, such as tissue engineering and drug delivery. Drug delivery systems (DDS) have shown several advantages over traditional drug therapy, such as greater therapeutic efficacy, prolonged delivery profile, and reduced drug toxicity, as evidenced by in vitro and in vivo studies as well as clinical trials. Despite that, there is no perfect delivery carrier, and issues such as undesirable viscosity and physicochemical stability or inability to efficiently encapsulate hydrophilic/hydrophobic molecules still persist, limiting DDS applications. To overcome that, biohybrid systems, originating from the synergistic assembly of polymers and other organic materials such as proteins and lipids, have recently been described, yielding molecularly planned biohybrid systems that are able to optimize structures to easily interact with the targets. This work revised the biohybrid DDS clarifying their advantages, limitations, and future perspectives in an attempt to contribute to further research of innovative and safe biohybrid polymer-based system as biomaterials for the sustained release of active molecules.

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Advances in Hybrid Polymer-Based Materials for Sustained Drug Release

The aim of this study was to formulate and evaluate in vitro, ceftriaxone sodium lipospheres dispersions for oral administration. Ceftriaxone sodium lipospheres were prepared by melt-emulsification using 30%w/w Phospholipon® 90H in Softisan® 154 as the lipid matrix containing increasing quantities of PEG 4000 (10, 20, 30, and 40%w/w). Characterization based on particle size, particle morphology, encapsulation efficiency, loading capacity and pH were carried out on the lipospheres. Microbiological studies of the ceftriaxone sodium-loaded lipospheres were performed using Escherichia coli as the model organism. In vitro permeation of ceftriaxone sodium from the lipospheres through artificial membrane (0.22 μm pore size) was carried out using Franz cell and simulated intestinal fluid (SIF) without pancreatin as acceptor medium. Photomicrographs revealed spherical particles within a micrometer range with minimal growth after 1 month (Maximum size = 64.76 ± 3.81 μm). Microbiological studies indicated that lipos...

O. Okorie

Papers

Formulation and in vitro evaluation of a PEGylated microscopic lipospheres delivery system for ceftriaxone sodium.

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