Traditional systemic chemotherapy involves the wide distribution of drug molecules in the body, causing toxic side effects in the healthy tissues and limiting the therapeutic dose required at the site of drug action. In order to decrease side effects and increase the drug efficacy, recent research on chemotherapy focuses on drug targeting. Targeted therapy can be achieved by several mechanisms including; 1) using an antibody as a drug that is specific to a disease biomarker, 2) using an antibody (or peptide) as a targeting agent conjugated to the drug molecule, 3) delivering the drug molecules to the target tissue in a nano-carrier with or without the targeting agent attached on its surface. The third approach involves the nanomedicines that can be targeted to diseased tissues by both passive (extravasating at diseased sites due to leaky vasculature) and active (specific interaction of the targeting agent with disease biomarker) targeting mechanisms. In this review we will cover the passively targeted nanomedicines prepared using nano drug carriers. Ideally the carrier particle should be in the right size (1-100nm), stable enough to prevent drug leakage during circulation, and safe not to cause any damage to healthy tissues. Competition for all these properties generated many different types of materials to be used as nanodrug delivery systems. After a brief review of most commonly used drug carriers, we discuss the clinical use of the targeted nanomedicines with regard to their pharmacokinetic and pharmacodynamics properties, and how these properties vary from conventional formulations providing free drugs in the circulation after administration.

The aim of this study was to design and optimize risperidone (RIS) mucoadhesive buccal tablets for systemic delivery as an alternative route. Direct compression method was used for the preparation of buccal tablets, and screening studies were conducted with different polymers to determine their effects on tablet characteristics. Carbopol® (CP) and sodium alginate (SA) were selected as two polymer types for further optimization studies by applying response surface methodology. Tablet hardness (TH), ex vivo residence time (RT), and peak detachment force (DF) from buccal mucosa were selected as three important responses. Physicochemical compatibility of formulation excipients and RIS was evaluated by using Fourier transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) analysis. In vitro drug release profiles and release kinetics were investigated; swelling index and matrix erosion studies were conducted. Optimum formulation consisted of 16.4% CP and 20.3% SA, which provided 7.67±0.29 hour ex vivo RT, 45.52±4.85 N TH, and 2.12±0.17 N DF. FT-IR spectroscopy and DSC analysis revealed that there was no chemical interaction present between tablet ingredients. Cumulative RIS release of >90% was achieved after 8 hours of in vitro dissolution studies, which was supported by swelling and matrix erosion analysis. Mechanism of RIS release was fitted best to zero-order model, while release exponent (n) value of 0.77 demonstrated an anomalous (non-Fickian) release, indicating combined erosion and swelling mechanism. The results suggested that optimized buccal tablets of RIS would be a promising and alternative delivery system for the treatment of schizophrenia.

Overall, HPMC was found to combine desired controlled release and mucoadhesion characteristics with sufficient pharmaceutical quality for optimization of buccal tablets. Piribedil mucoadhesive buccal tablets designed for the first time may introduce a new alternative for the treatment of Parkinson's disease.

Coenzyme Q10 (CoQ10) is a lipid-soluble molecule found naturally in many eukaryotic cells and is essential for electron transport chain and energy generation in mitochondria. D-Panthenyl triacetate (PTA) is an oil-soluble derivative of D-panthenol, which is essential for coenzyme A synthesis in the epithelium. Liposomal formulations that encapsulate both ingredients were prepared and optimized by applying response surface methodology for increased stability and skin penetration. The optimum formulation comprised 4.17 mg CoQ10, 4.22 mg PTA and 13.95 mg cholesterol per 100 mg of soy phosphatidylcholine. The encapsulation efficiency of the optimized formulation for CoQ10 and PTA was found to be 90.89%±3.61% and 87.84%±4.61%, respectively. Narrow size distribution was achieved with an average size of 161.6±3.6 nm, while a spherical and uniform shape was confirmed via scanning electron microscopy and transmission electron microscopy images. Cumulative release of 90.93% for PTA and 24.41% for CoQ10 was achieved after 24 hours of in vitro release study in sink conditions. Physical stability tests indicated that the optimized liposomes were suitable for storage at 4°C for at least 60 days. The results suggest that the optimized liposomal formulation would be a promising delivery system for both ingredients in various topical applications.

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In this review, therapeutic potential of drug delivery of SLN and nanostructured lipid carriers (NLC, the second generation of SLN) are summarized considering researches and patents on their administration via different routes and their preparations in the pharmaceutical market.

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