The objective of this work is to formulate and evaluate an emulgel containing calcipotriol for treatment of psoriasis. Emulgels have emerged as a promising drug delivery system for the delivery of ...hydrophobic drugs. Isopropyl alcohol and polyethylene glycol have been employed as permeation enhancers. Formulation chart is made with seven formulations, evaluated for physical parameters, drug content, viscosity, thixotropy, spreadability, extrudability, mucoadhesion, diffusion studies, skin irritation test along with short term stability studies. Carbopolis is reported to have a direct influence on appearance and viscosity of final formulation. The photomicroscopic evaluations showed the presence of spherical globules in size range of 10–15μm. Rheograms revealed that all the formulations exhibited pseudoplastic flow. Optimized formulation (F6) had shown 86.42±2.0% drug release at the end of 8h study. The release rate through dialysis membrane and rat skin is higher when compared to commercial calcipotriol ointment. Hence it is concluded that calcipotriol can be delivered topically with enhanced penetration properties when formulated as emulgel.
The aim of the study was to develop 5-FU loaded pH and thermo-sensitive nanogels, capable of sensing change in tumour environment pH and triggering drug release at physiological temperature. Poly(
N
...-isopropylacrylamide-
co
-acrylic acid) (PNA) nanogels (Ng's) were prepared
via
free radical polymerization. The prepared nanogels were screened for FT-IR,
1
H NMR, pH dependent lower critical solution temperature (LCST), and DLS. Selected Ng's were loaded with 5-FU and screened for FTIR, particle size, TEM, % EE,
in vitro
drug release, % hemolysis, pH dependent cytotoxicity,
in vivo
kinetics on Wistar rats,
in vivo
anti-cancer efficacy and mean life span on Swiss albino mice. FTIR and
1
H NMR confirmed the formation of PNA. The prepared nanogels exhibited pH dependent LCST. The particle size of selected PNA and 5-FU–PNA Ng's were found to be 70.25 and 131.5 nm respectively at 25 °C. Drug release from 5-FU–PNA Ng's was found to be extended and highly sustained at pH 5.5, 6.8 and 7.4. However, when compared with respect to individual pH, drug release in pH 7.4 PBS was quite minimal when compared to pH 5.5 and 6.8. The cytotoxicity of 5-FU–PNA Ng's increased with decrease in pH value. Additionally they could extend
in vivo
circulation time and displayed effective anti-cancer efficacy when compared to 5-FU injection for the same. Our results documented enhanced anti-cancer efficacy and mean life span in EAC bearing mice.
The aim of the study was to investigate potential of Solid Self Nano-Emulsifying Drug Delivery System (SNEDDS) for enhancing solubility and oral bioavailability of Rosuvastatin Calcium (RC). RC ...solubility was determined in different vehicles such as oils, surfactants and co-surfactants. Capmul MCM (oil), Tween 20 (surfactant) and PEG 200 were taken for the preparation of SNEDDS based upon the solubility of RC. Pseudo-ternary phase diagrams were constructed in order to identify efficient self-emulsifying regions. S-SNEDDS were prepared by adsorbing the optimized SNEDDS on to porous polystyrene spheres as a carrier. The S-SNEDDS formulated was free flowing and droplet size of the reconstituted nano-emulsion was almost unchanged after solidification. The prepared S-SNEDDS showed 98.92% release of RC at the end of 60 min, whereas pure RC exhibited only 38.6%. The C sub(max) and AUC sub(0-)t of the S-SNEDDS was about 7.97 and 7.91 fold higher than the pure drug respectively. This research study gives an overview of the S-SNEDDS as a hopeful choice to improve the oral bioavailability of RC.
The aim of the study was to develop and evaluate Polyelectrolyte complex (PEC) microparticles composing Lactobacillus Acidophilus (probiotic) and Fructo oligosaccharide-Lactobacillus Acidophilus ...(prebiotic-probiotic), for sustaining and enhancing intestinal growth of probiotic bacteria. Gum Karaya-Chitosan(GK-CH) was used to fabricate PEC microparticles by extrusion method. The prepared microparticles were characterized for FT-IR, DSC and particle size and evaluated for percentage yield, swelling, surface morphology, entrapment rate and further studied for influence of prebiotic over probiotic growth. The fabricated PEC microparticles composed of Probiotic and Prebiotic- Probiotic have exhibited sustainability of probiotic bacteria for 12 hrs in GIT conditions and presence of prebiotic in the preparation enhanced the probiotic cell growth. Hence, it can be concluded that PEC between GK-CH was found to be successful in sustaining cell release and presence of prebiotic was found to enhance the probiotic cell growth.
The aim of the present research was to develop Mannosylated Amphotericin B nanoparticles (AmB-BSA-MAN NPs) for targeting M-cells in Peyers patch to enhance drug transport across the intestinal ...epithelial barrier.
Bovine serum albumin (BSA) stabilized AmB NPs were prepared using liquid anti-solvent (LAS) precipitation technique, and different in process parameters were optimized using I-Optimal Response Surface Methodology. Lyophilized AmB-BSA NPs were crosslinked with mannose (MAN) via carbodiimide method using 1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDAC).
Prepared NPs were characterized using FT-IR, DSC, XRD, 1H NMR, SEM, and further evaluated for in vitro drug release, macrophage uptake and oral pharmacokinetics studies. FT-IR and 1H NMR results confirmed the compatibility as well as surface grafting of MAN. XRD studies outcomes revealed decreased crystallinity of AmB in the formulation. Fabricated AmB-BSA-MAN NPs were found to be irregular in shape; as confirmed by SEM. The particle size was found to be 303 nm and 352 nm for developed AmB-BSA NPs and AmB-BSA-MAN NPs, respectively. Further, the prepared NPs exhibited superior aqueous solubility and drug release when compared to its pure form. Further, in vitro macrophage uptake of AmB-BSA-MAN NPs in differentiated THP-1 cells was superior to AmB-BSA NPs and AmBisome®, but lesser than Fungizone®. The relative bioavailability of AmB from the prepared AmB-BSA-MAN NPs was found to be 793.2%; fairly higher in contrast to that from the plain AmB.
Our findings highlight the scope on developing new-fangled oral delivery system for passively targeting M-cells in Peyers patch for more competent and facilitated anti-leishmanial therapy.
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The aim of the present research was to improve the aqueous solubility and oral bioavailability of glibenclamide (GLB), a BCS class-II drug. A GLB nanosuspension (NS) was prepared using a liquid ...anti-solvent (LAS) precipitation technique and stabilized using HPMC K15M and lactose. Different in-process variables which directly affect the precipitated particle size have been thoroughly studied and optimized. The effect of a cryoprotective agent which could prevent agglomeration during lyophilisation was investigated. The optimal formulations of GD-H0.3d and GD-H0.4f exhibited a size range of 168.6 and 342.2 nm respectively and did not show any interaction when screened for incompatibility using FT-IR and DSC, but exhibited a decrease in crystallinity. The prepared GLB NPs exhibited superior aqueous solubility and dissolution when compared to pure GLB. The oral bioavailability of optimized formulations was found to exhibit 2.59, 1.67, 1.19, 2.50 and 2.40 folds of increment with respect to
C
max
,
K
el
(h
−1
),
t
1/2
, AUC
0–24 h
and AUC
0–∞
for GD-0.3d in contrast to pure GLB.
The aim of the study was to investigate potential of Solid Self Nano-Emulsifying Drug Delivery System (SNEDDS) for enhancing solubility and oral bioavailability of Rosuvastatin Calcium (RC). RC ...solubility was determined in different vehicles such as oils, surfactants and co-surfactants. Capmul MCM (oil), Tween 20 (surfactant) and PEG 200 were taken for the preparation of SNEDDS based upon the solubility of RC. Pseudo-ternary phase diagrams were constructed in order to identify efficient self-emulsifying regions. S-SNEDDS were prepared by adsorbing the optimized SNEDDS on to porous polystyrene spheres as a carrier. The S-SNEDDS formulated was free flowing and droplet size of the reconstituted nano-emulsion was almost unchanged after solidification. The prepared S-SNEDDS showed 98.92% release of RC at the end of 60 min, whereas pure RC exhibited only 38.6%. The
C
max
and AUC
0-
t
of the S-SNEDDS was about 7.97 and 7.91 fold higher than the pure drug respectively. This research study gives an overview of the S-SNEDDS as a hopeful choice to improve the oral bioavailability of RC.
The aim of the study was to investigate potential of Solid Self Nano-Emulsifying Drug Delivery System (SNEDDS) for enhancing solubility and oral bioavailability of Rosuvastatin Calcium (RC).
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