scholarly journals Development and Invitro Evaluation of Solid Lipid Nano Particles Loaded Topical Gel Containing Combination of Drugs Used In The Better Therapy of Psoriasis

2021 ◽  
Vol 11 (6) ◽  
pp. 21-33
Author(s):  
Suryakumari Chalakanti ◽  
Narender Malothu

The present research work was aimed to develop a Solid lipid nanoparticles (SLNs) based topical gel for the treatment of psoriasis. SLNs were prepared and then incorporated in a topical gel as a carrier. High-Pressure Homogenization method was used to improved drug loading capacity and drug release properties. Excipients like Compritol 888 ATO, Tween 80,Precirol ATO5, Poloxamer407, Cremophor RH40, Carpobol 934, Methyl Paraben, TEA, Distilled water were used. The optimized formulations were based on Zeta potential, analysis of particle size, differential scanning Colorimetery, scanning electron microscopy and study of Invitro drug release. The present research study revealed that the SLNs based Gel containing F4 formulation could potentially exploit as a carrier with improved drug loading capacity and drug release properties. Thus, tacrolimus loaded SLNs formulation can be beneficial in the treatment of psoriasis. It was concluded that the prepared formulation can be used for treatment of psoriasis by using the topical therapy of nanogel and this will attempt to increase the efficacy of the drug at the site of action.

2020 ◽  
Vol 10 (2) ◽  
pp. 20-25
Author(s):  
Ankita Kashyap ◽  
Asha Das ◽  
Abdul Baquee Ahmed

The present research work is based on the formulation and evaluation of topical gel of Ibuprofen where Carbopol 940 is used as the polymer. Gels were prepared by dispersing the polymers  in a mixture of water and glycerol with methyl paraben as the preservative and the varying amount of ibuprofen, being kept under magnetic stirring until the homogeneous dispersion was formed. The dispersion was then neutralized and made viscous by the addition of triethanolamine. The Carbopol gels of Ibuprofen were found to be homogenous with good drug loading. The pH of all the gel formulations was found within the neutral pH range which is compatible with skin. And the viscosity of the formulations was found to be feasible for topical drug delivery. The drug content of the three formulations was found in the range of 87.56% to 90.45% which shows efficient drug loading. Results of In vitro drug release study showed that F5 formulation has better diffusion of drug through egg membrane and hence further permeation studies were carried out through rat epidermis. The compatibility study showed that the major peaks in FTIR spectra of the pure drug were found to be intact in their physical mixture. Hence there is no interaction between drug and Carbopol in their physical mixture. Carbopol can be effectively used as the polymer for topical gel preparation. And F5 formulation containing 0.5 % w/w Carbopol 940 may be effectively used as topical transdermal delivery for Ibuprofen. Keywords: Ibuprofen, Transdermal Gel, Drug release, Compatibility study


2014 ◽  
Vol 3 (12) ◽  
pp. 331-335 ◽  
Author(s):  
Shumaia Parvin ◽  
Md. Abu Shuaib Rafshanjani ◽  
Md. Abdul Kader

Dexamethasone is a type of steroid medication having anti-inflammatory and immunosuppressant effects. One of the major problems with this drug is its low solubility in water which results into poor bioavailability after oral administration. So the objective of the present work is to improve the solubility and dissolution rate of dexamethasone using its solid lipid nano particles (SLNPs) with stearic acid as solid lipid, lutrol F-68 as surfactant and tween-80 as stabilizer. SLNPs are prepared by hot homogenization method at different ratio of drug, lipid, surfactant and stabilizer and designated as DNP1 to DNP6. In vitro dissolution study was performed using the USP type II apparatus (paddle method) at 50 rpm to a temperature of 37°±0.5°C in distilled water containing 0.75% w/v SLS (sodium lauryl sulfate). The absorbance of sample was measured spectrophotometrically at ?max 239nm on a UV-Visible spectrophotometer. Release pattern of drug was found to follow zero order, first order and Korsmeyer-Peppas equations. Improvement of dissolution was observed in all the solid lipid nano particles as compared to pure drug. Pure drug showed only 27.25% release in 50 min whereas the dexamethasone SLNPs showed faster (66.19%) in vitro drug release. Hence, this finding indicates that dexamethasone SLNPs prepared by hot homogenization method can be used to enhance the dissolution rate and to show novel application to this drug delivery system.DOI: http://dx.doi.org/10.3329/icpj.v3i12.20829 International Current Pharmaceutical Journal, November 2014, 3(12): 331-335


2019 ◽  
Author(s):  
Mahwish Kamran ◽  
Mir Azam Khan ◽  
Maqsood ur Rehman ◽  
Muhammad Shafique ◽  
Abdullah Khan ◽  
...  

Current study focused on resolution of poor oral bioavailability issues of cefixime through fabrication of its freeze dried binary solid lipid nano particles (SLNs). The nano formulation fabricated via hot melt encapsulation (HME) method was optimized using numerous formulation variables. Optimized nano formulation (CFX-4) showed particle size 206.6±2.3 nm, polydispersity index (PDI) 0.271±0.03, zeta potential (ZP) -30.7±3.1 mV, encapsulation efficiency (EE%) 88.2±2.3% along with drug loading capacity (DLC%) 4.83±0.16%. Micrograph of scanning electron microscopy (SEM) represented spherical shaped particles. Reduction in drug’s crystalline nature was acknowledged through differential scanning calorimetry (DSC) and x-ray powder diffraction (P-XRD) analysis. Drug-excepient compatibility was established through fourier transform infrared spectroscopic (FT-IR) analysis. During in-vitro studies; sustained drug release was favored by increased drug payload. Stability studies exposed that refrigerated temperature imparts maximum stability to binary SLNs. In-vivo pharmacokinetic studies revealed the desired enhancement in oral bioavailability compared to the marketed product (Cefiget®). Presented investigations established the dominance of binary SLNs for improvement of oral bioavailability with sustained drug release characteristics. Based on the reported outcomes, binary SLNs can be employed as an advanced drug delivery system for other hydrophobic drugs.


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


2019 ◽  
Vol 9 (3) ◽  
pp. 222-233
Author(s):  
Divya D. Jain ◽  
Namita D. Desai

Background: Adapalene is a promising third generation retinoid used in the topical treatment of acne vulgaris. However, the major drawback associated with conventional topical therapy of Adapalene is the ‘retinoid reaction’ which is dose-dependent and characterized by erythema, scaling and burning sensation at the application sites. Microparticulate drug delivery can play a major role in reducing side effects and providing better patient compliance due to targeted delivery. Methods: Adapalene microparticles were prepared using quasi emulsion solvent diffusion method. The effects of formulation variables including polymer ratios, amounts of emulsifier, drug loading and process variables such as stirring time and speed on the physical characteristics of microparticles were investigated. The developed microparticles were characterized by DSC and SEM. Adapalene microparticles were incorporated into Carbopol 971 NF gel for ease of topical delivery. Results: Adapalene microparticulate topical gel showed sustained drug release over 8 hours in in vitro studies. The amount of drug retained in the rat skin during ex vivo studies was higher in the microparticulate topical gel (227.43 ± 0.83 µg/cm2) as compared to the marketed formulation (81.4 ± 1.11 µg/cm2) after 8 hours indicating localized and sustained drug action that can be useful in treating acne vulgaris. The safety of optimized Adapalene gel determined by skin irritation studies performed on Sprague Dawley rats showed no irritation potential. Conclusion: Microparticles can provide promising carrier systems to deliver Adapalene, improving patient compliance due to enhanced skin deposition, localized and sustained action with reduced associated irritant effects.


2018 ◽  
Vol 6 (11) ◽  
pp. 61-80 ◽  
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma

In the present experimental investigation an attempt has been made to assess the utility of Crushed Puffed Rice (CPR)-High Molecular Weight Chitosan (HMWCH)-Hydroxypropyl Methylcellulose K15M (HPMC K15M) as a polymeric carrier for the sustained stomach delivery of Piroxicam (PRX). A total of nine formulations were prepared by using 3 (2) Taguchi factorial design, physically blending drug and polymer(s) followed by encapsulation into hard gelatin capsules size 1. The prepared capsules were evaluated for various performance such as weight variation, drug contents, in vitro buoyancy and drug release in 0.1 M HCl. The effect of drug loading on in vitro performance of the formulations was also determined. Crushed puffed rice (CPR) remained buoyant for up to average time span of 06 hr as an unwetted irregular mass in 0.1 M HCl. However, when combined with HMWCH or HPMC K15M or HPMC K15M + HMWCH a low -density cylindrical raft type hydrogel was formed which remained buoyant for up to 12 hr and released up to 99% drug in a sustained manner from 8 to 12 hr following zero order release kinetics. It was also observed that drug release from drug + CPR matrices followed Fickian mechanism. Combination of CPR + HMWCH or HMWCH + HPMC K15M also follows Fickian mechanism. Obtained data from the research work suggests that CPR in combination with HMWCH or HPMC K15M or HPMC has sufficient potential to be used as a carrier for stomach specific delivery of gastric irritant drug like PRX.Soni et al., International Current Pharmaceutical Journal, April 2018, 6(11): 61-80http://www.icpjonline.com/documents/Vol6Issue11/01.pdf


2018 ◽  
Vol 8 (5) ◽  
pp. 465-474
Author(s):  
S PADMA PRIYA ◽  
AN Rajalakshmi ◽  
P Ilaveni

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods:  Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine  formulations were formulated and  evaluated for  possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro  drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.


Author(s):  
Marwa H. Abdallah ◽  
Amr S. Abu Lila ◽  
Md. Khalid Anwer ◽  
El-Sayed Khafagy ◽  
Muqtader Mohammad ◽  
...  

The present work was aimed to develop a transferosomal gel of ibuprofen (IBU) for the amelioration of psoriasis like inflammation. Three formulation of IBU loaded transferosomes (TFs1-TFs3) were prepared using different proportions of lipid (phospholipon 90H) and surfactant (tween 80) and further evaluated for vesicle size, zeta potential (ZP), entrapment efficiency and in vitro drug release. The IBU loaded transferosomes (TFs2) was optimized with vesicle size (217±8.4 nm), PDI (0.102), ZP (-31.5±4.3 mV), entrapment efficiency (88.4±6.9%) and drug loading (44.2±2.9%). Further, the optimized IBU loaded transferosomes (TFs2) was incorporated into 1% carbopol 934 gel base and characterized for homogeneity, extrudability, viscosity and drug content. The in vivo pharmacodynamic study of gel exhibited reduction in psoriasis like inflammation in mice. The ibuprofen loaded transferosomal gel was successfully developed and has shown the potential to be a new therapy against psoriasis like inflammation.


Author(s):  
Veintramuthusankar Veintramuthusankar ◽  
Pushparajudayakumar Pushparajudayakumar ◽  
Rajanduraibabyroselin Rajanduraibabyroselin

Solid lipid nanoparticles (SLNs) are novel drug carrier system which consists of a solid matrix composed of a lipid being solid at both room and body temperatures with a mean Particle Size (PS) between 50 and 1000 nm Mupirocin -Tinidazole solid-lipid nanoparticles were prepared using hot homogenization technique using Glyceryl monosterate, Stearic acid, Tween 80 and Poloxamer 188 using hot homogenization technique. Size of the nanoparticles was in the range of 83 to 211 nm with the zeta potential values between -2.1 to -5.2. Atomic Force Microscopy (AFM) confirms the spherical shape of solid lipid nanoparticles. Entrapment efficiency was best in the F1 formulation. In vitro release of the pure drug was found to be 75% of mupirocin and 66.5% of tinidazole at the end of 1 hr. Drug release from SLNs dispersion followed Korsermeyrs peppas-model, indicating fickian diffusion drug release, while that from the gel followed non Fickian model drug release. Antibacterial activity of the SLNs was less but the SLNs based gel shows no significant difference in activity to that of standard drug gentamycin against aerobic bacteria. The SLNs dispersion exhibited physicochemical stability under refrigeration upto 45 days without significant difference in particle size. Best formulation was developed into a topical gel using sodium alginate and it was evaluated for pH, viscosity, spreadbility, extrudability, bloom strength, Minimum Inhibitory Concentration (MIC) and Methicillin resistant staphylococcus aureus (MRSA). Extrudability and spreadability parameters of the gel are similar to that of marketed Mupirocin 2% cream formulation


Author(s):  
Gayathri Hariharan ◽  
Priyanka Sinha

Objective: To optimize and evaluate the formulation of metronidazole (MT)-loaded chitosan microspheres and to investigate the efficiency of biodegradable polymer in developing sustained release formulation of MT to prolong the action of drug.Methods: MT microspheres were prepared using emulsion cross-linking method. Polymer-drug compatibility study was done using Fourier transform infrared. Physical characteristics were evaluated by particle size,SEM, flow properties etc. In vitro studies for evaluating drug release for MT-loaded chitosan microspheres were done by dissolution study.Results: Particle size of the formulated microspheres was found to be within the range of 110-130 μm. Flow properties of F1-F7 such as angle of repose, bulk density, and tapped density were found to be within limits. Drug entrapment efficiency was found to be better for all the formulations within the range of 74.82-84.32% w/w. Drug loading capacity was found to be in the range of 56-83.2% w/v. In vitro drug release was found to be in the range of 81.32-96.23% w/v.Conclusion: In spite of all the above results, we conclude that F5 formulation was optimized depending on the data obtained from the drug loading capacity and percentage drug release studies. F5 formulation is formulated with drug-polymer ratio 1:2 with 1% of di octyl sodium sulfo succinate and 8 ml of glutaraldehyde as a cross-linking agent.


Sign in / Sign up

Export Citation Format

Share Document