Publications by authors named "Awesh K Yadav"

17 Publications

  • Page 1 of 1

Therapeutic potential of nanoemulsions as feasible wagons for targeting Alzheimer's disease.

Drug Discov Today 2021 Jul 29. Epub 2021 Jul 29.

Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India. Electronic address:

Alzheimer's disease (AD) is an irreversible dementia state with characteristic clinical manifestations, including declining cognitive skills and loss of memory, which particularly affects the older population. Despite significant efforts in the field of nano-based drug delivery, there have been few successes achieved in the design of a rational drug therapy. Nanoemulsions (NEs) have potential for the delivery of AD therapeutics owing to their capability for brain drug delivery. Still, there is a long way to go before such therapeutics become a reality in the clinic. In this review, we highlight the preclinical assessment of NEs for AD and discuss the regulatory constraints to their clinical acceptance.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.drudis.2021.07.020DOI Listing
July 2021

Heparin appended ADH-anionic polysaccharide nanoparticles for site-specific delivery of usnic acid.

Int J Pharm 2019 Feb 27;557:238-253. Epub 2018 Dec 27.

Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics, Bhagyoday Tirth Pharmacy College, Sagar, Madhya Pradesh 470001, India. Electronic address:

The intention of present research work is to formulate usnic acid (UA) loaded heparin modified gellan gum (HAG) nanoparticles (NPs). HAG copolymer based conjugation was synthesized and characterized by H NMR and FT-IR spectroscopy. Plain and UA loaded HAG NPs were prepared via nanoprecipitation technique. NPs were typified and further characterized for particle size, polydispersity index, entrapment efficiency, zeta potential, atomic force microscopy, differential scanning calorimetry, X-ray diffraction analysis, and in-vitro release. In-vitro tube formation assay, tumorsphere assay, autophagy assay, DNA cleavage assay, internalization by confocal and FACS based internalization analysis, caspase assay and cell cycle assay were performed for biological activity. Obtained experimental results explored that HAG NPs displayed a sustained release of UA (95.67% in 48 h) compared to gellan gum NPs (96.12% in 8 h). In cytotoxicity studies, UA loaded HAG NPs exhibited an enormous cytotoxic potential against A549 cancer cells. In the in vivo bio-distribution study, using albino rat model the free UA concentration was found 7.09 ± 0.9%, 2.7 ± 1.5%, 7.5 ± 2.1, 9.2 ± 2%, and 6.25 ± 1.3% post two hours of intravenous administration, however, in the case of UA loaded HAG NPs the obtained level was 4.1 ± 1.10, 7.7 ± 1.30%, 2.21 ± 0.29%, 1.85 ± 0.25%, 2.2 ± 0.78%, 2.9 ± 1.21% respectively, in heart, lung, liver, spleen, intestine and kidney. The overall anticancer study and result of internalization deciphered the higher anticancer potential of UA loaded HAG NPs.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ijpharm.2018.12.049DOI Listing
February 2019

MCM-41 Nanoparticles for Brain Delivery: Better Choline-Esterase and Amyloid Formation Inhibition with Improved Kinetics.

ACS Biomater Sci Eng 2018 Aug 25;4(8):2860-2869. Epub 2018 Jul 25.

Bhagyoday Tirth Pharmacy College, Khurai Road, Sagar, Madhya Pradesh 470002, India.

The present study was aimed at delivering a low bioavailability drug, rivastigmine hydrogen tartrate (RTG), to the brain through its encapsulation in mesoporous silica nanoparticles (MSNs) and targeted to amyloid inhibition in the brain. MSNs were characterized for size, zeta potential, and drug entrapment using SEM, TEM, HR-TEM, FT-IR, and PXRD. Drug-loaded MSNs were assessed for in vitro release kinetics and ex vivo followed by animal studies. The average size of the prepared blank (MCM-41B) and drug-loaded MSNs (MCM-41L) was 114 ± 2.0 and 145 ± 0.4 nm with the zeta potential of approximately -43.5 ± 1.1 and -37.6 ± 1.4 mV, respectively. MCM-41L exhibited an average entrapment efficiency of 88%. In vitro release studies exhibited early surge followed by a sluggish persistent or constant release (biphasic pattern). Hemolytic studies proved that the developed MCM-41L NPs are less hemolytic compared to RTG. A reduced ThT fluorescence was observed with MCM-41L compared to MCM-41B and RTG in the amyloid inhibition studies. A significant ( < 0.05) inhibition of AChE (acetycholinesterase) was observed for MCM-41L (80 ± 4.98%), RTG (62 ± 3.25%), and MCM-41B (54 ± 4.25%). In vivo pharmacokinetics in Wistar rats revealed that the AUC and mean residence time (MRT) for MCM-41L was sustained and significantly higher ( < 0.05) (780 ± 3.30 ng/L; 5.49 ± 0.25 h) compared to RTG solution (430 ± 3.50 ng/L; 0.768 ± 0.17 h). Similarly, the half-life was found to be significantly higher in case of MCM-41L. The promising result was brain delivery of RTG in Wistar rats which was enhanced almost 127 folds in vivo, using MCM-41L nanoparticles. MCM-41L nanoparticles effectively enhanced the bioavailability of RTG. Conclusively, these can be used for the administration of RTG and other related low bioavailability drugs for improved brain delivery.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1021/acsbiomaterials.8b00335DOI Listing
August 2018

Heparin-Tailored Biopolymeric Nanocarriers in Site-Specific Delivery: A Systematic Review.

Crit Rev Ther Drug Carrier Syst 2017 ;34(1):1-33

Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics, Bhagyoday Tirth Pharmacy College, Sagar, M.P., India 470001.

The combination of nanocarriers and biological molecules is of intense interest because of the synergistic properties offered by such newly synthesized composites. Heparin conjugated to nanomaterials has recently been investigated for its beneficial chemical and biological properties and its capacity to improve the biocompatibility of nanocarriers, increasing their performance in various biological applications. A variety of recent research combines heparin and nanomaterials for a myriad of uses. For example, heparin has been conjugated to the surface of magnetic and metallic nanoparticles, biodegradable and nondegradable synthetic polymers, nanocomposites, dendrimers, and the like. It has also been incorporated into nanocarriers. There are numerous possibilities for material composites and chemistries that incorporate heparin. These open the door for a range of novel applications, including improving anticoagulant activity, anticancer and antitubercular therapy, tissue engineering, and biosensors. This review examines the different possibilities of heparin-based nanocarriers and their medicinal or biological applications.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1615/CritRevTherDrugCarrierSyst.2017016794DOI Listing
March 2017

Heparin-appended polycaprolactone core/corona nanoparticles for site specific delivery of 5-fluorouracil.

Artif Cells Nanomed Biotechnol 2017 Sep 4;45(6):1-10. Epub 2016 Jul 4.

c Nanotechnology Project Laboratories, Department of Pharmaceutics , Bhagyoday Tirth Pharmacy College , Sagar , Madhya Pradesh , India.

The aim of the present work is to formulate heparin-modified-polycaprolactone (HEP) core shell nanoparticles (NPs) of 5-fluorouracil (5-FU). These NPs were characterized for various in vitro parameters like particle size, zeta potential, etc. HEP NPs were found to maintain comparatively slower drug release pattern (98.9% in 96 h) than PCL NPs. Cytotoxicity studies demonstrated a massive cytotoxic potential of 5-FU-loaded HEP NPs in A549, MDA-MD-435, and SK-OV-3 cancer cell lines. Pharmacokinetic parameters were also determined in blood after IV administration of HEP NPs: AUC, C, MRT, and T values are 6096.075 ± 5.90 μg h/mL, 144.38 ± 1.52 μg/L, 58.71 ± 0.25 h, 96 ± 0.50 h, respectively and 117.92 ± 1.78, 45.35 ± 3.00, 1.2 ± 0.25, 0.5 ± 0.02 in plain 5-FU solution.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/21691401.2016.1203793DOI Listing
September 2017

Preliminary investigation for wound healing and anti-inflammatory effects of Bambusa vulgaris leaves in rats.

J Ayurveda Integr Med 2016 Mar 11;7(1):14-22. Epub 2016 Apr 11.

Department of Pharmacy, Guru Ramdas Khalsa Institute of Science and Technology, Jabalpur, Madhya Pradesh, India.

Background: Bambusa vulgaris (Family: Poaceae) used in Ayurveda for paralytic complaints, inflammatory disorders and externally to skin disorders. It has various medicinal uses with good nutritional composition and a rich source of vitamins, proteins, amino acid, beta-carotene and phenolic compounds.

Objective: The present study was aimed to evaluate wound healing and anti-inflammatory potential of ethanol extract of B. vulgaris leaves in rats.

Materials And Methods: The B. vulgaris leaves were evaluated for wound healing on incision and excision wound methods. Anti-inflammatory effect was evaluated by measurement of paw edema in carrageenan-induced inflammation in rats. Ethyl acetate (BVL-A) and aqueous (BVL-B) fractions from the ethanol extract of leaves were screened for wound healing effects by measuring tensile strength and biochemical parameters in incision wound method. The wound contraction area, antioxidant status and histopathological studies were done in excision wound method.

Results: Tensile strength and hydroxyproline level of 5% w/w ointment of BVL-A and BVL-B treated groups were found significantly (P < 0.01) higher and comparable to the reference group. The histopathological study showed the proliferation of collagen, fibrous tissue, and capillaries with epidermal covering at the margin of the wound. The percent inhibition of paw edema was significantly decrease by increasing concentration of BVL-A and BVL-B fractions. In addition, it was found that B. vulgaris possesses antioxidant properties, by its ability to increase antioxidants level.

Conclusions: The results obtained in the present study were indicated that ethyl acetate fraction of B. vulgaris leaves inhibits paw edema and accelerates cutaneous wound healing.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.jaim.2015.07.001DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4910292PMC
March 2016

Development and characterization of embelin-loaded nanolipid carriers for brain targeting.

Artif Cells Nanomed Biotechnol 2017 May 25;45(3):409-413. Epub 2016 Mar 25.

a Department of Pharmaceutics , I.S.F. College of Pharmacy , GT Road , Moga , Punjab , India.

The objective of present work was to enquire the potential use of embelin-loaded nanolipid carriers for brain targeting. The average particle size and polydispersity index (PDI) of optimized formulation (F19) were found to be 152 ± 19.7 nm and 0.143 ± 0.023, respectively. Nanolipid carrier (NLC) was also significantly attenuated pentylenetetrazole (PTZ)-induced biochemical parameters in comparison to plain embelin that results in an increase in the level of malondialdehyde (MDA), nitrite, and reduction in the level of glutathione. From the results, it was concluded that embelin-NLCs developed as a beneficial carrier to achieve sustained release and brain targeting through nasal route.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3109/21691401.2016.1160407DOI Listing
May 2017

Hyaluronic acid embedded cellulose acetate phthlate core/shell nanoparticulate carrier of 5-fluorouracil.

Int J Biol Macromol 2016 Jun 5;87:449-59. Epub 2016 Mar 5.

Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics, Guru Ramdas Khalsa Institute of Science and Technology Pharmacy, Kukrikheda, Barela 482003, Madhya Pradesh, India. Electronic address:

Aim of this research was to prepare hyaluronic acid-modified-cellulose acetate phthalate (HAC) core shell nanoparticles (NPs) of 5-fluorouracil (5-FU). HAC copolymer was synthesized and confirmed by fourier transform infrared (FTIR) and nuclear magnetic resonance (NMR) spectroscopy. HAC NPs with 5-FU were prepared using HAC copolymer and compared with 5-FU loaded cellulose acetate phthalate (CAP) NPs. NPs were characterized by atomic force microscopy (AFM), particle size, zeta potential, polydispersity index, entrapment efficiency, in-vitro release, differential scanning calorimetry (DSC) and X-ray diffraction (XRD). HAC NPs were found slower release (97.30% in 48h) than (99.25% in 8h) CAP NPs. In cytotoxicity studies, showed great cytotoxic potential of 5-FU loaded HAC NPs in A549, MDA-MD-435 and SK-OV-3 cancer cellline. HAC NPs showing least hemolytic than CAP NPs and 5-FU. Area under curve (AUC), maximum plasma concentration (Cmax), mean residence time (MRT) and time to reach maximum plasma concentration Tmax), were observed 4398.1±7.90μgh/mL, 145.45±2.25μg/L, 45.74±0.25h, 72±0.50h, respectively of HAC NPs and 119.92±1.78μgh/mL, 46.38±3.42μg/L, 1.2±0.25h, 0.5±0.02h were observed in plain 5-FU solution. In conclusion, HAC NPs is effective deliver carrier of 5-FU for lung cancer.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ijbiomac.2015.11.094DOI Listing
June 2016

Enteric-coated epichlorohydrin crosslinked dextran microspheres for site-specific delivery to colon.

Drug Dev Ind Pharm 2015 26;41(12):2018-28. Epub 2015 May 26.

a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , India.

Enteric-coated epichlorohydrin crosslinked dextran microspheres containing 5-Fluorouracil (5-FU) for colon drug delivery was prepared by emulsification-crosslinking method. The formulation variables studied includes different molecular weights of dextran, volume of crosslinking agent, stirring speed, time and temperature. Dextran microspheres showed mean entrapment efficiencies ranging between 77 and 87% and mean particle size ranging between 10 and 25 µm. About 90% of drug was released from uncoated dextran microspheres within 8 h, suggesting the fast release and indicated the drug loaded in uncoated microspheres, released before they reached colon. Enteric coating (Eudragit-S-100 and Eudragit-L-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method. The release study of 5-FU from coated dextran microspheres was complete retardation in simulated gastric fluid (pH 1.2) and once the coating layer of enteric polymer was dissolved at higher pH (7.4 and 6.8), a controlled release of the drug from the microspheres was observed. Further, the release of drug was found to be higher in the presence of dextranase and rat caecal contents, indicating the susceptibility of dextran microspheres to colonic enzymes. Organ distribution and pharmacokinetic study in albino rats was performed to establish the targeting potential of optimized formulation in the colon.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3109/03639045.2015.1044901DOI Listing
August 2016

In-vitro and in-vivo assessment of dextran-appended cellulose acetate phthalate nanoparticles for transdermal delivery of 5-fluorouracil.

Drug Deliv 2016 Jun 24;23(5):1525-35. Epub 2014 Nov 24.

a Drug Delivery and Nanotechnology Laboratories, Department of Pharmaceutics , Guru Ramdas Khalsa Institute of Science and Technology Pharmacy Kukrikheda , Barela , Madhya Pradesh , India.

The aim of this research was transdermal delivery of 5-fluorouracil (5-FU) using dextran-coated cellulose acetate phthalate (CAP) nanoparticulate formulation. CAP nanoparticles were prepared using drug-polymer ratio (1:1 to 1:3) and surfactant ratio (2.5, 5 and 10%). Dextran coating was made using aminodextran. The results showed that the optimized CAP nanoparticles (CNs) and dextran-coated CAP nanoparticles represented core-corona nanoparticles with the mean diameter of 75 ± 3 and 79 ± 2 nm, respectively, and entrapment efficiency was 82.5 ± 0.06 and 78.2 ± 0.12, respectively. Dextran-coated nanoparticles (FDCNs) and CAP nanoparticles (FCNs) showed in vitro 5-FU release upto 31 h and 8 h, respectively. Moreover, the cumulative amount of 5-FU penetrated through excised skin from FDCNs was 2.94 folds than that of the FU cream. Concentration of 5-FU in epidermis and dermis were also studied. In dermis, concentration of 5-FU was found higher in case of FDCN formulation than plain FU cream. FDCNs were found more hemocompatible in comparison to FCNs. The hematological data recommended that FDCNs formulation was less immunogenic compared to FU creams formulation. In blood level study, FDCNs exhibited 153, 12, 16.66 and 16.24-fold higher values for area under the curve, Tmax, Cmax and mean residence time (MRT) compared with those of FU cream, respectively. The in-vitro cytotoxicity was assessed using the MCF-7 by the MTT test and was compared to the plain 5-FU solution. All the detailed evidence showed that FDCNs could provide a promising tuning as a transdermal delivery system of 5-FU.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3109/10717544.2014.978512DOI Listing
June 2016

Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon.

Drug Deliv 2016 20;23(1):328-37. Epub 2014 May 20.

a Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences , Dr. Hari Singh Gour University , Sagar , Madhya Pradesh , India.

Objective of the present investigation was to prepare and evaluate the potential of enteric coated dextran microspheres for colon targeting of 5-fluorouracil (5-FU). Dextran microspheres were prepared by emulsification-crosslinking method and the formulation variables studied included different molecular weights of dextran, drug:polymer ratio, volume of crosslinking agent, stirring speed and time. Enteric coating (Eudragit S-100) of dextran microspheres was performed by oil-in-oil solvent evaporation method using different coat:core ratios (4:1 or 8:1). Uncoated and coated dextran microspheres were characterized by particle size, surface morphology, entrapment efficiency, DSC, in vitro drug release in the presence of dextranase and 2% rat cecal contents. The release study of 5-FU from coated dextran microspheres was pH dependent. No release was observed at acidic pH; however, the drug was released quickly where Eudragit starts solublizing there was continuous release of drug from the microspheres. Organ distribution study was suggested that coated dextran microspheres retard the release of drug in gastric and intestinal pH environment and released of drug from microspheres in colon due to the degradation of dextran by colonic enzymes.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3109/10717544.2014.913733DOI Listing
October 2016

Chondroitin sulphate decorated nanoparticulate carriers of 5-fluorouracil: development and in vitro characterization.

J Biomed Nanotechnol 2010 Aug;6(4):340-50

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University Sagar (M.P.) 470003, India.

The present study investigates prospective of tailored nanoparticles as vectors to provide improved therapeutic efficacy of encapsulated anti-cancer drug 5-FU. Condritin Sulphate (CS) conjugated PLGA nanoparticles were prepared using PEG-bis-amine and adipic dihydrazide as spacers and loaded with an anti-cancer drug 5-FU (CS-PEG-PLGA-FU and CS-ADH-PLGA-FU). The formulations were then compared with non CS-anchored monomethoxy(polyethylene glycol) (MPEG-PLGA-FU) nanoparticles. Nanoparticlulate systems were further characterized by FTIR, NMR, TEM studies and particle size/polydispersity index (PDI) analysis. DSC and XRD were also performed to assess the nature of 5-FU inside the nanoparticles. The nanoparticles prepared using amphiphilic block copolymer CS-PEG-PLGA were able to sustain the release of 5-FU up to 48 h whereas those of CS-ADH-PLGA and MPEG-PLGA released the drug up to 24 h. The CS-PEG-PLGA-FU nanoparticles were found to be least haemolytic when compared to free drug, CS-ADH-PLGA-FU and MPEG-PLGA-FU nanoparticles. Cytotoxicity studies were performed on MCF-7/MDA-MD 231 breast cancer cells. PLGA nanoparticles exhibited more potent cytotoxic effect on MCF-7/MDA-MD 231 cells than free doxorubicin. Further, enhanced cytotoxicity and lower hemolytic potential of CS-PEG-PLGA-FU nanoparticles suggest a potential application in cancer chemotherapy.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1166/jbn.2010.1118DOI Listing
August 2010

Development and characterization of hyaluronic acid decorated PLGA nanoparticles for delivery of 5-fluorouracil.

Drug Deliv 2010 Nov;17(8):561-72

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H. S. Gour University, Sagar, India.

The present investigation was aimed to develop and explore the prospective of engineered PLGA nanoparticles as vehicles for targeted delivery of 5-fluorouracil (5-FU). Nanoparticles of 5-FU-loaded hyaluronic acid-poly(ethylene glycol)-poly(lactide-co-glycolide) (HA-PEG-PLGA-FU) copolymer were prepared and characterized by FTIR, NMR, transmission electron microscopy, particle size analysis, DSC, and X-ray diffractometer measurement studies. The nanoparticulate formulation was evaluated for in vitro release, hemolytic toxicity, and hematological toxicity. Cytotoxicity studies were performed on Ehrlich ascites tumor (EAT) cell lines using MTT cell proliferation assay. Biodistribution studies of 99m Tc labeled formulation were conducted on EAT-bearing mice. The in vivo tumor inhibition study was also performed after i.v. administration of HA-PEG-PLGA-FU nanoparticles. The HA conjugated formulation was found to be less hemolytic but more cytotoxic as compared to free drug. The hematological data suggested that HA-PEG-PLGA-FU formulation was less immunogenic compared to plain drug. The tissue distribution studies displayed that HA-PEG-PLGA-FU were able to deliver a higher concentration of 5-FU in the tumor mass. In addition, the HA-PEG-PLGA-FU nanoparticles reduced tumor volume significantly in comparison with 5-FU. Thus, it was concluded that the conjugation of HA imparts targetability to the formulation, and enhanced permeation and retention effect ruled out its access to the non-tumor tissues, at the same time favored selective entry in tumors, thereby reducing the side-effects both in vitro and in vivo.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.3109/10717544.2010.500635DOI Listing
November 2010

An insight on hyaluronic acid in drug targeting and drug delivery.

J Drug Target 2008 Feb;16(2):91-107

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr Hari Singh Gour University, Sagar, India.

Hyaluronic acid (HA) has recently been studied for its use in drug delivery applications. Medically, HA is used as a surgical aid in ophthalmology. It also possesses therapeutic potential in the treatment of arthritis and wound healing. HA-binding receptors, CD44 and receptor for hyaluronan-mediated motility have attracted much enthusiasm, mainly because they are believed to be involved in cancer metastasis. This review unravels the role of HA in drug delivery and targeting. Designing of various novel drug delivery systems using HA as a biopolymer will also be reviewed in the present article.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/10611860802095494 DOI Listing
February 2008

Microsphere based improved sunscreen formulation of ethylhexyl methoxycinnamate.

Curr Drug Deliv 2007 Apr;4(2):153-9

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar-470 003, India.

Polymethylmethacrylate (PMMA) microspheres of ethylhexyl methoxycinnamate (EHM) were prepared by emulsion solvent evaporation method to improve its photostability and effectiveness as sunscreening agent. Process parameters like stirring speed and aqueous polyvinyl alcohol (PVA) concentration were analyzed in order to optimize the formulations. Shape and surface morphology of the microspheres were examined using scanning electron microscopy. Particle size of the microspheres was determined using laser diffraction particle size analyzer. The PMMA microspheres of EHM were incorporated in water-removable cream base. The in vitro drug release of EHM in pH 7.4 was performed using dialysis membrane. Thin layer chromatography was performed to determine photostability of EHM inside the microspheres. The formulations were evaluated for sun protection factor (SPF) and minimum erythema dose (MED) in albino rats. Cream base formulation containing microspheres prepared using EHM:PMMA in ratio of 1:3 (C(3)) showed slowest drug (EHM) release and those prepared with EHM: PMMA in ratio of 1:1 showed fastest release. The cream base formulations containing EHM loaded microspheres had shown better SPF (more than 16.0) as compared to formulation C(d) that contained 3% free EHM as sunscreen agent and showed SPF 4.66. These studies revealed that the incorporation of EHM loaded PMMA microspheres into cream base had greatly increased the efficacy of sunscreen formulation approximately four times. Further, photostability was also shown to be improved in PMMA microspheres.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.2174/156720107780362285DOI Listing
April 2007

Eudragit-coated pectin microspheres of 5-fluorouracil for colon targeting.

AAPS PharmSciTech 2007 Feb 16;8(1):12. Epub 2007 Feb 16.

Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar, India.

An objective of the present investigation was to prepare and evaluate Eudragit-coated pectin microspheres for colon targeting of 5-fluorouracil (FU). Pectin microspheres were prepared by emulsion dehydration method using different ratios of FU and pectin (1:3 to 1:6), stirring speeds (500-2000 rpm) and emulsifier concentrations (0.75%-1.5% wt/vol). The yield of preparation and the encapsulation efficiencies were high for all pectin microspheres. Microspheres prepared by using drug:polymer ratio 1:4, stirring speed 1000 rpm, and 1.25% wt/vol concentration of emulsifying agent were selected as an optimized formulation. Eudragit-coating of pectin microspheres was performed by oil-in-oil solvent evaporation method using coat:core ratio (5:1). Pectin microspheres and Eudragit-coated pectin microspheres were evaluated for surface morphology, particle size and size distribution, swellability, percentage drug entrapment, and in vitro drug release in simulated gastrointestinal fluids (SGF). The in vitro drug release study of optimized formulation was also performed in simulated colonic fluid in the presence of 2% rat cecal content. Organ distribution study in albino rats was performed to establish the targeting potential of optimized formulation in the colon. The release profile of FU from Eudragit-coated pectin microspheres was pH dependent. In acidic medium, the release rate was much slower; however, the drug was released quickly at pH 7.4. It is concluded from the present investigation that Eudragit-coated pectin microspheres are promising controlled release carriers for colon-targeted delivery of FU.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1208/pt0801012DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2750447PMC
February 2007

Preparation and characterization of oxybenzone-loaded gelatin microspheres for enhancement of sunscreening efficacy.

Drug Deliv 2006 Sep-Oct;13(5):323-30

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. Hari Singh Gour University, Sagar, India.

The objective of our present study was to prepare and evaluate gelatin microspheres of oxybenzone to enhance its sunscreening efficacy. The gelatin microspheres of oxybenzone were prepared by emulsion method. Process parameters were analyzed to optimize the formulation. The in vitro drug release study was performed in pH 7.4 using cellulose acetate membrane. Microspheres prepared using oxybenzone:gelatin ratio of 1:6 showed slowest drug release and those prepared with oxybenzone:gelatin ratio of 1:2 showed fastest drug release. The gelatin microspheres of oxybenzone were incorporated in aloe vera gel. Sun exposure method using sodium nitroprusside solution was used for in vitro sunscreen efficacy testing. The formulation C5 containing oxybenzone-bearing gelatin microspheres in aloe vera gel showed best sunscreen efficacy. The formulations were evaluated for skin irritation test in human volunteers, sun protection factor, and minimum erythema dose in albino rats. These studies revealed that the incorporation of sunscreening agent-loaded microspheres into aloe vera gel greatly increased the efficacy of sunscreen formulation more than four times.
View Article and Find Full Text PDF

Download full-text PDF

Source
http://dx.doi.org/10.1080/10717540500398175DOI Listing
November 2006
-->