Preparation and standardizations of structural nano- lipid loaded lidocaine and conventional lidocaine (original) (raw)
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Formulation and Evaluation of Lidocaine Lipid Nanosystems for Dermal Delivery
AAPS PharmSciTech, 2009
The objective of the present investigation was to formulate solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) for improving the dermal delivery of a local anesthetic agent lidocaine (LID). SLN and NLC were characterized for particle size distribution, polydispersity index, entrapment efficiency, X-ray powder diffraction pattern (XRD), thermal behavior by differential scanning colorimeter (DSC) and surface morphology by transmission electron microscopy (TEM). LID-loaded SLN and NLC were formulated into hydrogels for topical application. The in vitro permeation profiles of LID SLN gel, LID NLC gel, and a marketed LID formulation (Xylocaine® gel) were evaluated by using guinea pig skin. The in vivo efficacy of LID SLN gel, LID NLC gel, and a marketed LID formulation (Xylocaine® gel) gel was evaluated on guinea pig using pinprick test. LID SLN showed a particle size of 78.1 nm with a polydispersity index of 0.556, whereas LID NLC showed a particle size of 72.8 nm with a polydispersity index of 0.463. The entrapment efficiency of LID in both SLN and NLC was 97% and 95.9%, respectively. The TEM studies revealed the almost spherical nature of LID SLN and NLC formulations. The XRD and DSC studies of LID SLN suggested amorphization of drug in the carrier system. The SLN formulation was stable with respect to particle size, polydispersity, and entrapment efficiency for 6 months at 40°C/75% relative humidity (RH). Negligible leakage was observed for the NLC formulation when stored for 1 month at 40°C/75% RH. In vitro permeation studies indicated that LID SLN gel and LID NLC gel significantly sustained the LID release compared to that of Xylocaine® gel. The in vivo efficacy results supported the results of the in vitro permeation studies wherein the LID SLN gel and LID NLC gel resulted in fivefold and sixfold increase in duration of anesthesia, respectively, compared to that of Xylocaine® gel.
International Journal of Nanoscience, 2021
Lidocaine is a primary local anesthesia that blocks the ionic fluxes required for the beginning and operation of impulses in the neuronal membrane. The benefits of local anesthetics, such as enhancing patient acceptance, prohibiting systemic toxicity and delivering continuous drug delivery, make them the attracting field for pharmaceutical researchers. The nanoparticles were prepared by solvent evaporation W1/O/W2 emulsion method and in the ratios of 1 to 1, 1 to 2 and 1 to 3 drug to polymer. The production yield, loading efficiency, particle size, poly dispersity index and zeta potential of selected formulation were 84.30%, 80.60%, 192[Formula: see text]nm, 0.18[Formula: see text]mV and [Formula: see text][Formula: see text]mV, respectively. DSC and FTIR studies showed that no chemical interactions between drug and polymer Formulations showed an initial burst release, which is a reason for the good capacity of the polymer to maintain the drug in it and lead to a primary slow release.
Journal of Pharmaceutical Sciences, 2011
The present study concerns the in vitro and in vivo evaluation of benzocaine (BENZO) and lidocaine (LIDO) topical delivery from nanostructured lipid carriers (NLCs). Morphology and dimensional distribution of NLCs have been, respectively, characterized by differential scanning calorimetry (DSC) and photon correlation spectroscopy. The release pattern of BENZO and LIDO from NLCs was evaluated in vitro determining drug percutaneous absorption through excised human skin. Radiant heat tail-flick test was carried out in mice to determine the antinociceptive effect of BENZO and LIDO from NLC. DSC studies revealed that the inner oil phase of NLC plays a significant role in stabilizing the particle architecture and increasing the drug solubility. In vitro evidences show that BENZO and LIDO, when incorporated in viscosized NLC dispersions, exhibited a lower flux with respect to formulations containing the free drugs in the aqueous phase. In vivo study enabled to demonstrate that BENZO and LIDO can be released in a prolonged fashion when incorporated into lipid carriers. The results obtained pointed out NLC capability to act as an effective drug reservoir, thus prolonging the anesthetic effect of BENZO and LIDO.
Lidocaine loaded biodegradable nanospheres
Journal of Controlled Release, 1999
The mechanism of the release of encapsulated lidocaine from spherical nanoparticles based on poly(D,L-lactic acid) polymer carrier (PLA) was studied through mathematical modelling. The drug was incorporated in the PLA matrix with particle sizes from approximately 250 to 820 nm and corresponding loadings varying from about 7 to 32% (w / w). The rate of release correlated with the particle drug loading and was fastest at small particles with a low drug content. It was about four times slower at large particles with a high loading when the process of release took up to 100 h. Two simple models, diffusion and dissolution, were applied for the description of the experimental data of lidocaine release and for the identification of the release mechanisms for the nanoparticles of different drug loading. The modelling results showed that in the case of high drug loadings (about 30% w / w), where the whole drug or a large part of it was in the crystallised form, the crystal dissolution could be the step determining the release rate. On the other hand, the drug release was diffusion-controlled at low loadings (less than 10% w / w) where the solid drug was randomly dispersed in the matrix. The estimated values of the 220 2 diffusion coefficient of lidocaine in these particles were in the range of 5-7310 m / s. A significant influence of both crystal dissolution and drug diffusion on the overall rate of release was assumed at PLA nanoparticles with medium lidocaine loadings.
Liposomal-Based Lidocaine Formulation for the Improvement of Infiltrative Buccal Anesthesia
Journal of liposome research, 2018
This study describes the encapsulation of the local anesthetic lidocaine (LDC) in large unilamellar liposomes (LUV) prepared in a scalable procedure, with hydrogenated soybean phosphatidylcholine, cholesterol and mannitol. Structural properties of the liposomes were assessed by dynamic light scattering (DLS), nanoparticle tracking analysis (NTA), and transmission electron microscopy (TEM). A modified, two-compartment Franz-cell system was used to evaluate the release kinetics of LDC from the liposomes. The in vivo anesthetic effect of liposomal lidocaine 2% (LUV) was compared to lidocaine 2% solution without (LDC) or with the vasoconstrictor epinephrine (1:100000) (LDC), in rat infraorbital nerve blockade model. The structural characterization revealed liposomes with spherical shape, average size distribution of 250 nm and low polydispersity even after LDC incorporation. Zeta potential laid around -30 mV and the number of suspended liposomal particles was in the range of 10 vesicles...
X-ray structures and pharmacological activities of lidocaine derivatives
Structural Chemistry, 2008
The molecular and crystal structures of the lidocaine analogs 2-(pyrazol-1-yl)-2′-methylacetanilide (1), 2-(3,5-dimethyl-4-iodo-pyrazol-1-yl)-2′-methylacetanilide (2), 2-(3,5-dimethyl-4-iodo-pyrazol-1-yl)-3′-methylacetanilide (3), and 2-(pyrazol-1-yl)-4′-methylacetanilide (4), are reported, with a summary of their pharmacological activities. In this series, the moiety comprising the heterocyclic ring and the amide alkyl linker displays a common conformation. Molecules of 1–4 form identical hydrogen bonded motifs in their crystals, namely linear chains via intermolecular N–H···O=C hydrogen bonding. Moderate anesthetic and anti-arrhythmic potencies recorded for 1–4 relative to lidocaine are countered by their significantly lower toxicities.
Nanoethosomes for Dermal Delivery of Lidocaine
Advanced Pharmaceutical Bulletin, 2015
It is necessary for local anesthetics to pass through the stratum corneum to provide rapid pain relief. Many techniques have been reported to enhance intradermal penetration of local anesthetics such as vesicular lipid carriers. Ethosomes are lipid vesicles containing phospholipids, ethanol at relatively high concentration. We hypothesized that synergistic effects of phospholipids and high concentration of ethanol in formulation could accelerate penetration of nanoethosomes in deep layers of skin. Methods: Lidocaine-loaded nanoethosomes were prepared and characterized by size and zeta analyzer, scanning electron microscopy (SEM) and X-ray diffractometer (XRD). Furthermore, encapsulation efficiency (EE), loading capacity (LC), and skin penetration capability were evaluated by in vitro and in vivo experiments. Results: results showed that the particle size, zeta potential, EE and LC of optimum formulation were 105.4 ± 7.9 nm,-33.6 ± 2.4 mV, 40.14 ± 2.5 %, and 8.02 ± 0.71 respectively. SEM results confirmed the non-aggregated nano-scale size of prepared nanoethosomes. Particle size of ethosomes and EE of Lidocaine were depended on the phospholipid and ethanol concentrations. XRD results demonstrated the drug encapsulation in amorphous status interpreting the achieved high drug EE and LC values. In vitro and in vivo assays confirmed the appropriate skin penetration of Lidocaine with the aid of nanoethosomes and existence of deposition of nanoethosomes in deep skin layers, respectively. Conclusion: The developed nanoethosomes are proposed as a suitable carrier for topical delivery of anesthetics such as Lidocaine.
Formulation and Evaluation of Lidocaine Hydrochloride Chewable Tablet
Asian Journal of Pharmaceutical and Clinical Research
Objective: The objective of this study was to formulate and optimize a chewable formulation of lidocaine hydrochloride using a 32 factorial design for optimized the superdisintegrant concentration.Methods: Various concentrations of sodium starch glycolate (SSG) (13.33 mg, 26.66 mg, and 40 mg) of superdisintegrant and starch (50 mg, 83 mg, and 116.66 mg) were added in the formulation; nine formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. The models were tested for significance. Procedure to manufacture chewable tablets by direct compression was established.Results: The results show that the presence of a superdisintegrant is desirable for chewable formulation. The best-optimized batch F7 found the batch having starch of amount 116.66 mg and SSG 13.33 mg. All the prepared batches of tablets were within t...
Journal of Drug Delivery Science and Technology
The aim of this work was the formulation and comparison of different drug carrier systems for the transdermal delivery of lidocaine. Quality target product profile and quality attributes were identified, and an initial risk assessment was made according to the Quality by Design methodology. The critical quality attributes influencing the quality and efficacy of the final drug formulation were then defined in order to select the control points and proper methods for measurements. Four formulation types, each containing 5 % lidocaine were compared: conventional hydrogel, oleogel, lyotropic liquid crystal and nanostructured lipid carrier. Microscopic analysis, particle size and zeta potential measurements, Fourier transform infrared spectroscopy and Raman spectroscopy were performed to characterize the critical parameters in case of the different vehicles. Membrane diffusion and penetration studies were completed as well for each formulation in vitro and ex vivo, followed by measurements on skin hydration and transepidermal water loss in vivo. Our results lead us to the conclusion that the nanostructured lipid carrier is the most promising vehicle for the topical delivery of lidocaine. It showed the best penetration properties through heat separated epidermis and the highest moisturizing effect which are the most critical parameters based on the Quality by Design initial risk assessment and evaluation.