The drug delivery system using solid lipid nanoparticles (SLN) came into being about two decades ago and since then lot of work has been done in this field.1-5) SLN for oral drug administration are specifically used to target the uptake of the drug by lymphatic system which prevents its first pass metabolism. Lymphatic uptake of drugs follow two routes which include transcellular transport through the enterocyte and phagocytosis of the drugs by Mast cells of payer's patches lining the intestinal mucosa. [6][7][8] The production of this nano particulate system is based on the principle of solidification of lipid nano emulsion.9) The different technologies available for the fabrication of SLN are high shear homogenization, ultrasound, high pressure homogenization (cold homogenization and hot homogenization), solvent emulsification/evaporation and microemulsion method.10) The major excipients used in the development of the SLN are fatty acids, mono, di and triglycerides, phospholipids etc., which are part of the physiological composition and thus are biocompatible to the body. [11][12][13] SLN have been shown to have superior advantages over polymeric nanoparticles, fat emulsion and liposomes.14) SLN can be produced on large scale and are also biocompatible to the body as compared to polymers, the monomeric unit of which are cytotoxic to the body.15,16) SLN exhibit sustained release effect due to the immobility of drug within lipid as compared to the emulsion formulations 17) and also exhibit better physical and chemical stability of drug compared to liposome.18) This delivery system has been extensively used as carriers for proteins, protein drugs, vaccines and lipophilic water insoluble drugs. 19) SLN are potential delivery system for lipophilic drugs where aqueous solubility of the drug is the limiting factor for its absorption. [20][21][22] Moreover, the incorporation of such drugs within SLN is easier due to their affinity for the lipid. On the other hand, entrapment of hydrophilic drug inside the hydrophobic matrix of SLN is a real challenge as the drug has maximum tendency to partition in the water during the fabrication process. Although a few hydrophilic molecules have been incorporated into SLN like thymocratin, 23) insulin, 24) diminazene 25) and thymopentin, 26) lot more scope still remains for the entrapment of hydrophilic drugs into lipid nanoparticles.Zidovudine (AZT), a hydrophilic drug has been used in the present investigation. It belongs to the class of nucleoside reverse transcriptase inhibitor and is used in the treatment of AIDS. This drug has various disadvantages like short biological half life due to extensive first pass metabolism and dose related bone marrow toxicity. AZT is a potential candidate for delivery via lipid based nanoparticulate system as this would help to improve lymphatic uptake, avoid hepatic first pass metabolism and thus reduce the dose requirement and decrease the side effects. 27) Furthermore, sustained drug release would reduce dosing frequency and at the same time ma...
The aim of the paper was to develop satranidazole-containing mucoadhesive gel for the treatment of periodontitis. Different mucoadhesive gels were prepared, using various gelling agents like sodium carboxymethylcellulose (SCMC), poloxamer 407, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, and the mucoadhesive polymer carbopol 934P. The selected formulations (based on the mucoadhesive force) were studied for different mechanical properties, such as mucoadhesive strength, hardness, compressibility, adhesiveness, and cohesiveness through Texture Profile Analyzer. In vitro satranidazole release from the prepared formulations was also determined and compared with marketed preparation of metronidazole (Metrogyl gel). The formulation SC30 (containing SCMC 3% w/v) showed maximum mucoadhesive strength (167.72 +/- 3.76 g) and adhesiveness (-46.23 +/- 0.34 N mm), with low hardness (9.81 +/- 0.04 N) and compressibility (40.05 +/- 0.48 N mm) and moderate cohesiveness (0.87 +/- 0.01). SC30 formulation exhibited long-term release. Thus, SC30 gel was evaluated for its clinical effectiveness along with marketed metronidazole gel. At the end of the study (42 days of clinical studies), both formulations were found to significantly reduce the probing depth, plaque index, gingival index, calculus criteria, and bleeding index. However, the SC30 gel was more effective in reducing the above parameters than marketed metronidazole gel. This study confirmed the acceptability and effectiveness of satranidazole gel for treatment of periodontitis.
The aim of the present research work was to develop asenapine (ASM) loaded nanostructured lipid carriers (ANLC) for the delivery of drugs in the brain by an intranasal route to enhance therapeutic efficacy.
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