In the golden age of pharmaceutical nanocarriers, we are witnessing a maturation stage of the original concepts and ideas. There is no doubt that nanoformulations are extremely valuable tools for drug delivery applications; the current challenge is how to optimize them to ensure that they are safe, effective and scalable, so that they can be manufactured at an industrial level and advance to clinical use. In this context, lipid nanoparticles have gained ground, since they are generally regarded as non-toxic, biocompatible and easy-to-produce formulations. Pharmaceutical applications of lipid nanocarriers are a burgeoning field for the transport and delivery of a diversity of therapeutic agents, from biotechnological products to small drug molecules. This review starts with a brief overview of the characteristics of solid lipid nanoparticles and discusses the relevancy of performing systematic preformulation studies. The main applications, as well as the advantages that this type of nanovehicles offers in certain therapeutic scenarios are discussed. Next, pharmacokinetic aspects are described, such as routes of administration, absorption after oral administration, distribution in the organism (including brain penetration) and elimination processes. Safety and toxicity issues are also addressed. Our work presents an original point of view, addressing the biopharmaceutical aspects of these nanovehicles by means of descriptive statistics of the state-of-the-art of solid lipid nanoparticles research. All the presented results, trends, graphs and discussions are based in a systematic (and reproducible) bibliographic search that considered only original papers in the subject, covering a 7 years range (2013-today), a period that accounts for more than 60% of the total number of publications in the topic in the main bibliographic databases and search engines. Focus was placed on the therapeutic fields of application, absorption and distribution processes and current efforts for the translation into the clinical practice of lipid-based nanoparticles. For this, the currently active clinical trials on lipid nanoparticles were reviewed, with a brief discussion on what achievements or milestones are still to be reached, as a way of understanding the reasons for the scarce number of solid lipid nanoparticles undergoing clinical trials.

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Solid Lipid Nanoparticles for Drug Delivery: Pharmacological and Biopharmaceutical Aspects

Preclinical safety of solid lipid nanoparticles and nanostructured lipid carriers: Current evidence from in vitro and in vivo evaluation.

Development of nanoparticles from natural lipids for topical delivery of thymol: Investigation of its anti-inflammatory properties.

Curcumin loaded nanostructured lipid carriers for enhanced skin retained topical delivery: optimization, scale-up, in-vitro characterization and assessment of ex-vivo skin deposition.

Tacrolimus and curcumin co-loaded liposphere gel: Synergistic combination towards management of psoriasis

Aim: The primary aim of present work was to develop effective combination drug therapy for topical treatment of psoriasis.Methods: Betamethasone dipropionate and calcipotriol loaded solid lipid nanoparticles (CT-BD-SLNs) were prepared by hot melt high shear homogenization technique, which were then incorporated in Carbopol gel matrix. The anti-psoriatic potential was tested by sequential in vitro (skin permeation and dermal distribution, anti-proliferative effect in HaCaT cells) and in vivo (Draize patch irritation, transepidermal water loss (TEWL) and anti-psoriatic mouse tail studies) experiments.Results: A negligible amount in receptor compartment, yet confined distribution of drugs to epidermal and dermal region of skin was observed in case of SLNs, which is essential for safe and effective anti-psoriatic therapy. Draize patch test and TEWL demonstrated negligible skin irritation and better skin tolerability of SLNs. The in vitro HaCaT cell line study demonstrated that SLNs delayed the abrupt growth o...

Solid lipid nanoparticles-loaded topical gel containing combination drugs: an approach to offset psoriasis

Biodegradation and biocompatibility are crucial for developing long-acting implantable drug delivery systems. Because of the prolonged biological residence of these implants, understanding of in vivo degradation and biocompatibility helps establish the commercial success of these implants. International Organization for Standardization has laid down various guidelines for the development and optimization of in vitro degradation studies. This chapter discusses multiple ISO guidelines and current research to understand the influence of different study parameters on biodegradation study. The chapter also summarizes the immunological consideration in the design and evaluation of long-acting implants.

Safety, biodegradability, and biocompatibility considerations of long-acting drug delivery systems

Anti-glaucoma latanoprost-loaded ocular implants provide prolonged delivery and enhanced bioavailability relative to the conventional eye drops. This study aims at the development and validation of a reversed-phase high-performance liquid chromatography method for quantitative analysis of nanogram levels of latanoprost in the eye, and for the first time, compares the use of fluorescence vs ultraviolet (UV) detectors in latanoprost quantification. The mobile phase was composed of acetonitrile:0.1% v/v formic acid (60:40, v/v) with a flow rate of 1 mL/min and separation was done using a C18 column at temperature 40°C. The fluorescence excitation and emission wavelengths were set at 265 and 285 nm, respectively, while the UV absorption was measured at 200 nm. The latanoprost concentration-peak area relationship maintained its linearity (R2 = 0.9999) over concentration ranges of 0.063-10 μg/mL and 0.212-10 μg/mL for the fluorescence and UV detectors, respectively. The UV detector showed better precision, while the fluorescence detector exhibited higher robustness and greater sensitivity, with a detection limit of 0.021 μg/mL. The fluorescence detector was selected for quantification of latanoprost released from ocular implants in vitro and in porcine ocular tissues. The developed method is a robust, rapid and cost-effective alternative to liquid chromatography-mass spectrometry for routine analysis of latanoprost released from ocular implants.

Latanoprost Quantification in Ocular Implants and Tissues: HPLC-Fluorescence vs HPLC-UV

https://pureadmin.qub.ac.uk/ws/files/169818969/Accepted_manuscript_v_3_Open_access_verison_.pdf

A validated size exclusion chromatography method coupled with fluorescence detection for rapid quantification of bevacizumab in ophthalmic formulations.

Rahul Sonawane

Papers

Solid lipid nanoparticles-loaded topical gel containing combination drugs: an approach to offset psoriasis

Safety, biodegradability, and biocompatibility considerations of long-acting drug delivery systems

Latanoprost Quantification in Ocular Implants and Tissues: HPLC-Fluorescence vs HPLC-UV

A validated size exclusion chromatography method coupled with fluorescence detection for rapid quantification of bevacizumab in ophthalmic formulations.

Mucoadhesive Nanocarriers for Nasal Delivery of Vaccines