scholarly journals Liposomal and Ethosomal Gels for the Topical Delivery of Anthralin: Preparation, Comparative Evaluation and Clinical Assessment in Psoriatic Patients

Pharmaceutics ◽  
2020 ◽  
Vol 12 (5) ◽  
pp. 446 ◽  
Author(s):  
Dina Fathalla ◽  
Eman M. K. Youssef ◽  
Ghareb M. Soliman

To enhance anthralin efficacy against psoriasis and reduce its notorious side effects, it was loaded into various liposomal and ethosomal preparations. The nanocarriers were characterized for drug encapsulation efficiency, size, morphology and compatibility between various components. Optimum formulations were dispersed in various gel bases and drug release kinetics were studied. Clinical efficacy and safety of liposomal and ethosomal Pluronic®F-127 gels were evaluated in patients having psoriasis (clinicaltrials.gov identifier is NCT03348462). Safety was assessed by recording various adverse events. Drug encapsulation efficiency ≥97.2% and ≥77% were obtained for liposomes and ethosomes, respectively. Particle sizes of 116 to 199 nm and 146 to 381 nm were observed for liposomes and ethosomes, respectively. Fourier-Transform infrared (FT-IR) spectroscopy and differential scanning calorimetry (DSC) studies confirmed the absence of interaction between anthralin and various nanocarrier components. Tested gel bases showed excellent ability to sustain drug release. At baseline, the patients had a median Psoriasis Area and Severity Index (PASI) of 3.4 for liposomes and 3.6 for ethosomes without significant difference. After treatment, mean PASI change was −68.66% and −81.84% for liposomes and ethosomes, respectively with a significant difference in favor of ethosomes. No adverse effects were detected in both groups. Anthralin ethosomes could be considered as a potential treatment of psoriasis.

Author(s):  
P M Jamkar ◽  
K N Gujar ◽  
S B Nemmaniwar ◽  
N B Kulkarni

Controlled drug release system is one of the most favourable technique of novel drug delivery system owing to its reproducibility and ease of formulation. Nanotechnology is very useful for controlling the drug release and thus improving the pharmacokinetic and pharmacodynamic properties of the drug. The technique improves patient compliance by reducing both dose and the frequency of administration and thus minimizing the local as well as systemic toxic effects. The aim of the present research work was to formulate and evaluate gastroretentive nanoparticles of Repaglinide, an anti-diabetic drug by using the ionotropic gelation method. Repaglinide has a very short half-life of 1 hour with bioavailability 56%. Sustained release mucoadhesive nanoparticles of Repaglinide were prepared to increase the drug residence time in gastrointestinal tract and thus improving the bioavailability of drug. The mucoadhesive nanoparticles were prepared by using chitosan and sodium alginate as polymers; calcium chloride as the crosslinking agent. Different formulations were prepared with varying concentrations of chitosan and sodium alginate in order to achieve the optimum particle size and maximum encapsulation efficiency. The particle size of nanoparticles was found to be in the range of 300 nm to 756 nm. Drug encapsulation efficiency ranged between 56% to 80% with controlled drug release upto 88% in phosphate buffer pH 7.4 and 75% drug release in 0.1N HCl in 12 hrs. FT-IR and DSC studies showed that the drug and polymers were compatible. The results of swelling study and bioadhesive strength indicated that optimized formulation exhibited excellent mucoadhesive properties


Author(s):  
Santosh G Gada ◽  
ANANDKUMAR Y. ◽  
C. MALLIKARJUN SETTY

Objective: The objective of this study was to design and evaluate controlled release mucoadhesive microspheres of lamivudine using mucoadhesive polymers and mucilage. Methods: Mucoadhesive microspheres of lamivudine were formulated by ionic gelation method. The response surface methodology was adapted for optimization of formulation using central composite design (CCD) for two factors at three levels each was employed to study the effect of independent variables, Sodium alginate-drumstick mucilage (X1) and calcium chloride (CaCl2) concentration (X2) on dependent variables, namely drug encapsulation efficiency (DEE) and particle size (PS). Optimized drumstick mucilage mucoadhesive microspheres of lamivudine were obtained by using numerical optimization of desirability approach. The observed microspheres were coincided well with the predicted values by the experimental design. Results: The microspheres formed were spherical in shape, and Particle size (PS) ranged between 681.63-941.57μm. Drug encapsulation efficiency (DEE) was ranged between 69.63-94.56 %. The drug release for an optimized formulation was 96.58 %. The mechanism of drug release from microspheres followed Korsemeyer’s-Peppas and exponential ‘n’ value was greater than 0.45, indicating the drug release was non-fickian i.e., swelling followed by erosion mechanism. Conclusion: This work suggests that mucoadhesive microspheres, an effective drug delivery system for lamivudine, can be prepared using drumstick mucilage in improving the bioavailability of the drug.


Author(s):  
Antony V. Samrot ◽  
SenthilKumar P. ◽  
Shashi Bhushan ◽  
Rishi Kurup ◽  
Ujjala Burman ◽  
...  

In this study, curcumin (CUR) was encapsulated into chitosan (CS) and carboxymethyl cellulose (CMC) microparticles using sodium tripolyphosphate (TPP) as chelator. Here, different concentrations (0.1%, 0.3% and 0.5%) of sodium tripolyphosphate (TPP) were utilised to synthesise microparticles. Microparticles were characterized by Fourier Transform Infra-Red Microscopy (FTIR) and Scanning Electron Microscope (SEM). All the CUR encapsulated microparticles were analysed for their drug encapsulation efficiency and the drug release kinetics. Microparticles were studied for the invitro controlled drug release against Pseudomonas aeruginosa.


Author(s):  
Bipul Nath ◽  
Santimoni Saikia

In the present investigation, sodium alginate based multiparticulate system overcoated with time and pH dependent polymer was studied in the form of oral pulsatile system to achieve pulsatile with sustained release of aceclofenac for chronotherapy of rheumatoid arthritis seven batches of micro beads with varying concentration of sodium alginate (2-5 %) were prepared by ionotropic-gelation method using CaCl2 as cross-linking agent. The prepared Ca-alginate beads were coated with 5% Eudragit L100 and filled into pulsatile capsule with varying proportion of plugging materials. Drug loaded microbeads were investigated for physicochemical properties and drug release characteristics. The mean particle sizes of drug-loaded microbeads were found to be in the range 596±1.1 to 860 ± 1.2 micron and %DEE in the range of 65-85%. FT-IR and DSC studies revealed the absence of drug polymer interactions. The release of aceclofenac from formulations F1 to F7 in buffer media (pH 6.8) at the end of 5h was 65.6, 60.7, 55.7, 41.2, 39.2, 27 and 25% respectively. Pulsatile system filled with eudragit coated Ca-alginate microbeads (F2) showed better drug content, particle size, surface topography, in-vitro drug release in a controlled manner. Different plugging materials like Sterculia gum, HPMC K4M and Carbopol were used in the design of pulsatile capsule. The pulsatile system remained intact in buffer pH 1.2 for 2 hours due to enteric coat of the system with HPMCP. The enteric coat dissolved when the pH of medium was changed to 7.4. The pulsatile system developed with Sterculia gum as plugging material showed satisfactory lag period when compared to HPMC and Carbopol.


2020 ◽  
Vol 17 (3) ◽  
pp. 246-256
Author(s):  
Kriti Soni ◽  
Ali Mujtaba ◽  
Md. Habban Akhter ◽  
Kanchan Kohli

Aim: The intention of this investigation was to develop Pemetrexed Diacid (PTX)-loaded gelatine-cloisite 30B (MMT) nanocomposite for the potential oral delivery of PTX and the in vitro, and ex vivo assessment. Background: Gelatin/Cloisite 30 B (MMT) nanocomposites were prepared by blending gelatin with MMT in aqueous solution. Methods: PTX was incorporated into the nanocomposite preparation. The nanocomposites were investigated by Fourier Transmission Infra Red Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Scanning Electron Microscope (SEM) X-Ray Diffraction (XRD) and Confocal Laser Microscopy (CLSM). FT-IR of nanocomposite showed the disappearance of all major peaks which corroborated the formation of nanocomposites. The nanocomposites were found to have a particle size of 121.9 ± 1.85 nm and zeta potential -12.1 ± 0.63 mV. DSC thermogram of drug loaded nanocomposites indicated peak at 117.165 oC and 205.816 oC, which clearly revealed that the drug has been incorporated into the nanocomposite because of cross-linking of cloisite 30 B and gelatin in the presence of glutaraldehyde. Results: SEM images of gelatin show a network like structure which disappears in the nanocomposite. The kinetics of the drug release was studied in order to ascertain the type of release mechanism. The drug release from nanocomposites was in a controlled manner, followed by first-order kinetics and the drug release mechanism was found to be of Fickian type. Conclusion: Ex vivo gut permeation studies revealed 4 times enhancement in the permeation of drug present in the nanocomposite as compared to plain drug solution and were further affirmed by CLSM. Thus, gelatin/(MMT) nanocomposite could be promising for the oral delivery of PTX in cancer therapy and future prospects for the industrial pharmacy.


Soft Matter ◽  
2018 ◽  
Vol 14 (27) ◽  
pp. 5622-5627 ◽  
Author(s):  
Isabel M. Bjørge ◽  
Ana M. S. Costa ◽  
A. Sofia Silva ◽  
João P. O. Vidal ◽  
J. Miguel Nóbrega ◽  
...  

Straight-forward production of spheroidal particles allows the assessment of the impact of geometry on cell encapsulation viability and drug release kinetics.


2020 ◽  
pp. 096739112090447
Author(s):  
O Sreekanth Reddy ◽  
MCS Subha ◽  
T Jithendra ◽  
C Madhavi ◽  
K Chowdoji Rao

This article reports the fabrication of pH-sensitive microbeads from sodium alginate (SA) and modified karaya gum (KG). KG was modified by graft copolymerization using 2-hydroxyethyl methacrylate (2-HEMA) through in situ free radical polymerization reaction. The graft copolymer was blended with SA to develop microbeads by a simple ionotropic gelation technique. The microbeads were characterized by Fourier transform infrared spectroscopy, X-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, and scanning electron microscopy. The effect of %HEMA and polymer blend ratio on the swelling capacity was investigated. Drug release kinetics of the microbeads was investigated under both pH 7.4 and pH 1.2 at 37°C. The drug release kinetics was analyzed by evaluating the release data using different kinetic models.


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