scholarly journals Excipients, drug release mechanism and physicochemical characterization methods of Solid lipid nanoparticles

2021 ◽  
Vol 11 (1-s) ◽  
pp. 139-146
Author(s):  
Vasu Deva Reddy Matta

From last thirty years, solid lipid nanoparticles (SLNs) gain much importance as drug delivery vehicle for enhanced delivery of the drugs, proteins, nutraceuticals and cosmetics. SLNs defined as a submicron size range nanoparticle with below 1000 nm and are mainly composed of lipids and surfactants, capable of incorporating both lipophilic and hydrophilic drugs. SLNs also used as controlled systems, targeted delivery and altered therapeutic efficacy purpose. A wide variety of methods such as double emulsion, solvent evaporation, ultra sonication, high-pressure homogenization and microemulsion used for SLNs production. This review provides the significance of SLNs in drug delivery with highlighting on selection of excipients, drug release mechanism, principles and limitations associated with their physicochemical and surface morphological characterization. Keywords: Solid lipid nanoparticles, enhanced delivery, preparation, characterization, application.

Author(s):  
Pravin Patil ◽  
Anil Sharma ◽  
Subhash Dadarwal ◽  
Vijay Sharma

The objective of present investigation was to enhance brain penetration of Lamivudine, one of the most widely used drugs for the treatment of AIDS. This was achieved through incorporating the drug into solid lipid nanoparticles (SLN) prepared by using emulsion solvent diffusion technique. The formulations were characterized for surface morphology, size and size distribution, percent drug entrapment and drug release. The optimum rotation speed, resulting into better drug entrapment and percent yield, was in the range of 1000-1250 r/min. In vitro cumulative % drug release from optimized SLN formulation was found 40-50 % in PBS (pH-7.4) and SGF (pH-1.2) respectively for 10 h. After 24 h more than 65 % of the drug was released from all formulations in both mediums meeting the requirement for drug delivery for prolong period of time.


Author(s):  
Sonia Pandey ◽  
Farhinbanu Shaikh ◽  
Arti Gupta ◽  
Purnima Tripathi ◽  
Jitendra Singh Yadav

Solid lipid nanoparticles are one of the developed technologies for addressing the bioavailability and targeting issues of drug delivery. In this review article, we attempted to incorporate all the essential details of SLNs like various methods of preparation, different models of SLNs, updated characterization methods, in-vivo behavior (Uptake), their applications, route of administration as well as advancements taken place in the field of delivery of biological drugs like gene vector, new adjuvant for vaccines, protein, and peptide with SLNs. Surface modified SLNs hold excellent potential for targeted and controlled drug delivery which is discussed and summarized. Based on the available data, the future success of SLNs is widened because they could be easily fabricated with various functionalities which would display enormous potential for targeting and diagnosing various diseases. This review would help the budding researchers to find out the unexplored areas of SLNs with the present discussion that reframes the potential of SLNs by gathering the various research findings of SLNs in tabular form along with the approved patent technologies of SLNs.


2021 ◽  
Vol 11 (1-s) ◽  
pp. 162-169
Author(s):  
Vasu Deva Reddy Matta

Solid lipid nanoparticles (SLNs) are in submicron size range nanoparticles and are made of biocompatible and biodegradable materials (mainly composed of lipids and surfactants) capable of incorporating both lipophilic and hydrophilic drugs. SLNs are also considered as substitute to other colloidal drug systems, also used as controlled systems and targeted delivery. SLNs can be considered as an alternative for oral drug delivery vehicle to improve the oral bioavailability of drugs, associated reduction of drug toxicity and stability of drug in both GIT and plasma. There are different techniques used for the preparation of SLNs. Generally, the preparation of SLNs and any other nanoparticle system necessitates a dispersed system as precursor; otherwise particles are produced through the use of a particular instrumentation. This review provides the summary on the techniques or methods used for the development of SLNs of poorly water soluble drugs for improved drug delivery. Keywords: Solid lipid nanoparticles, controlled delivery, precursor, techniques.


Author(s):  
Narendar Dudhipala

This article describes the current state and future perspectives of solid lipid nanoparticles for achieving high delivery of drugs with greater therapeutic outcomes.  The oral route is the most preferred route of administration for majority of drugs. Problems such as poor solubility or chemical stability in the environment of the gastrointestinal tract, poor permeability through the biological membranes or sensitivity to metabolism are well known to result in the rejection of potential drug candidates as oral delivery products. Hence, lipid-based drug delivery systems have been proposed as a means of bypassing the resistant chemical or physical barriers associated with poorly absorbed drugs. Solid lipid nanoparticles (SLNs) can be an attractive one option for oral drug delivery vehicles as they hold tremendous potential to improve the oral bioavailability of drugs, concomitant reduction of drug toxicity and stability of drug in both GIT and plasma. SLNs are in submicron size range and are made of biocompatible and biodegradable materials capable of incorporating both lipophilic and hydrophilic drugs. SLNs are considered as substitute to other colloidal drug systems and are being used as controlled and targeted delivery systems. The SNL technology has greatly revolutionized the delivery systems for poorly soluble drugs. This article describes the methodologies used for preparation and characterization of SNLs.  It outlined the development of stable solid lipid nanoparticles by different techniques. Further, it describes the current status of pharmacokinetic and pharmaco-dynamic studies reported on SLN systems. Finally, it provides a brief outlook on current marketed preparation and the future scope of SLN technology.


Author(s):  
S. Pragati ◽  
S. Kuldeep ◽  
S. Ashok ◽  
M. Satheesh

One of the situations in the treatment of disease is the delivery of efficacious medication of appropriate concentration to the site of action in a controlled and continual manner. Nanoparticle represents an important particulate carrier system, developed accordingly. Nanoparticles are solid colloidal particles ranging in size from 1 to 1000 nm and composed of macromolecular material. Nanoparticles could be polymeric or lipidic (SLNs). Industry estimates suggest that approximately 40% of lipophilic drug candidates fail due to solubility and formulation stability issues, prompting significant research activity in advanced lipophile delivery technologies. Solid lipid nanoparticle technology represents a promising new approach to lipophile drug delivery. Solid lipid nanoparticles (SLNs) are important advancement in this area. The bioacceptable and biodegradable nature of SLNs makes them less toxic as compared to polymeric nanoparticles. Supplemented with small size which prolongs the circulation time in blood, feasible scale up for large scale production and absence of burst effect makes them interesting candidates for study. In this present review this new approach is discussed in terms of their preparation, advantages, characterization and special features.


Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis


2016 ◽  
Vol 12 (5) ◽  
pp. 598-604 ◽  
Author(s):  
Tatiana N. Pashirova ◽  
Tatiana Andreani ◽  
Ana S. Macedo ◽  
Eliana B. Souto ◽  
Lucia Ya. Zakharova

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