Objectives One of the thrust areas in drug delivery research is transdermal drug delivery systems (TDDS) due to their characteristic advantages over oral and parenteral drug delivery systems. ...Researchers have focused their attention on the use of microneedles to overcome the barrier of the stratum corneum. Microneedles deliver the drug into the epidermis without disruption of nerve endings. Recent advances in the development of microneedles are discussed in this review for the benefit of young scientists and to promote research in the area.
Key findings Microneedles are fabricated using a microelectromechanical system employing silicon, metals, polymers or polysaccharides. Solid coated microneedles can be used to pierce the superficial skin layer followed by delivery of the drug. Advances in microneedle research led to development of dissolvable/degradable and hollow microneedles to deliver drugs at a higher dose and to engineer drug release. Iontophoresis, sonophoresis and electrophoresis can be used to modify drug delivery when used in concern with hollow microneedles. Microneedles can be used to deliver macromolecules such as insulin, growth hormones, immunobiologicals, proteins and peptides. Microneedles containing ‘cosmeceuticals’ are currently available to treat acne, pigmentation, scars and wrinkles, as well as for skin tone improvement.
Summary Literature survey and patents filled revealed that microneedle‐based drug delivery system can be explored as a potential tool for the delivery of a variety of macromolecules that are not effectively delivered by conventional transdermal techniques.
The present study was designed to formulate and develop fast disintegrating pellets of poorly soluble model drug (cilostazol) by reducing the proportion of micro-crystalline cellulose with ...pre-gelatinized starch (PGS), lactose and chitosan. The bioavailability enhancement of a model drug was achieved by preparing inclusion complex with Captisol® (Sulfobutyl Ether β cyclodextrin - SBE-β-CD). Extrusion-spheronization technique was used to formulate pellets. Placket-Burman design was used for the initial screening of most significant factors such as screen size (mm), ratio of micro crystalline cellulose: PGS + lactose + chitosan and % of HPMC which affects pellet properties. The inclusion complex of drug and Captisol
®
(SBE-β-CD) was prepared by Solvent Evaporation method and were incorporated into pellets in a predefined proportion. Formulation was optimized by using 3
2
full factorial design, the optimized batch was selected on the basis of dependent variables such as % yield, pellet size, disintegration time and % Cumulative drug release (%CDR), the obtained results were 87.15%, 0.75 mm, 13 min and 91.024% respectively. Differential scanning calorimetry (DSC) and Fourier transform infrared spectrometry (FTIR) study revealed no significant interaction between drug and polymer. Scanning electron microscopy (SEM) confirmed uniform and spherical shaped pellets having pores on the surface which facilitates wicking action and fast disintegrating property of pellets. A design space was constructed to meet the desirable target and optimized batch. The scope of study can further extended to hydrophobic molecules which may useful due to rapid disintegration and enhanced dissolution rate.
Long acting parenteral formulations are preferred over conventional formulations for the treatment of chronic diseases. Prevalence of such diseases provoked the interest of researchers and ...pharmaceutical industries in the development of long acting parenteral formulations. The regulatory guidelines and pharmacopoeia have remained silent on dissolution methods for long acting parenteral formulations due to their diverse nature. The lack of compendial method for dissolution testing increases the duration of approval process for long acting parenteral formulations. This article reviews various dissolution methods used to study in vitro drug release profile of long acting parenteral formulations. Compendial as well as noncompendial methods, such as- rotating dialysis cell, dialysis tube, rotating bottle, shaking flask, single drop, inverted cup and incubation, are used by researchers for drug release profile of long acting parenteral formulations. This review article also highlights the advantages and disadvantages of reported dissolution methods along with the suitability of these methods for particular type of long acting formulation. The compiled work will help the researchers in designing the biorelevant dissolution method and expedite the development of long acting parenteral formulations.
A accurate, precise and robust isocratic HPLC method has been developed and validated for simultaneous determination of Rifampicin and Ofloxacin. The chromatographic separation was carried out on ...Kinetex C
18
, 100 A Phenomenex column with a mixture of 0.03M Potassium dihydrogen phosphate buffer pH 3.0: Acetonitrile (55:45) as mobile phase at 230 nm. The retention times were 2.91 and 4.87 min for Ofloxacin and Rifampicin, respectively. Calibration plots were linear over the concentration range 1-5 and 2-10 µg/ml for Rifampicin and Ofloxacin, respectively. The method was validated for linearity, sensitivity accuracy, precision, and robustness. Percent recoveries were found to be close to 100% with low variability. Fractional factorial design with four factors was chosen for robustness testing. The volume of acetonitrile and flow rate showed significant effect on retention factor of both the drugs and asymmetry factor of ofloxacin. The method may be adopted for routine analysis at industry.
The aim of the present investigation was to evaluate microemulsion as a vehicle for dermal drug delivery and to develop microemulsion-based gel of terbinafine for the treatment of onychomycosis. ...D-optimal mixture experimental design was adopted to optimize the amount of oil (
X
1
), Smix (mixture of surfactant and cosurfactant;
X
2
) and water (
X
3
) in the microemulsion. The formulations were assessed for globule size (in nanometers;
Y
1
) and solubility of drug in microemulsion (in milligrams per milliliter;
Y
2
). The microemulsion containing 5.75% oil, 53.75% surfactant–cosurfactant mixture and 40.5% water was selected as the optimized batch. The globule size and solubility of the optimized batch were 18.14 nm and 43.71 mg/ml, respectively. Transmission electron microscopy showed that globules were spherical in shape. Drug containing microemulsion was converted into gel employing 0.75%
w
/
w
carbopol 934P. The optimized gel showed better penetration and retention in the human cadaver skin as compared to the commercial cream. The cumulative amount of terbinafine permeated after 12 h was 244.65 ± 18.43 μg cm
−2
which was three times more than the selected commercial cream. Terbinafine microemulsion in the gel form showed better activity against
Candida albicans
and
Trichophyton rubrum
than the commercial cream. It was concluded that drug-loaded gel could be a promising formulation for effective treatment of onychomycosis.
Background
Diabetes is undoubtedly one of the most challenging health problems in 21
st
century. Understanding the pathogenesis and preventing long term complications have been major goals of ...research in diabetes mellitus (DM). Research in the past few years has linked oxidative stress and inflammation to beta cell dysfunction. Aim of this study is to evaluate serum gamma-glutamyl transferase (GGT) activity (marker of oxidative stress) and high sensitivity C reactive protein (hsCRP) level (an inflammatory marker) in type 2 DM subjects with good and poor glycemic control. Further, we investigated correlation between serum GGT and hsCRP level with glycemic control (FBS, PP
2
BS, HbA
1
c) in subjects.
Methods
A cross sectional study consists of 150 patients out of them 50 patients having type 2 DM with good control (Group II), 50 patients with type 2 DM with poor control (Group III) and 50 normal healthy control (Group I) were selected. Serum GGT, serum hsCRP, FBS, PP
2
BS, HbA
1
c, and other biochemical investigations include serum liver enzymes and lipids were measured.
Results
Mean serum GGT and hsCRP concentration were statistically significantly higher in group III patients compared to group I and group II subjects as well as increased in group II compared to group I (p < 0.001). Further significant positive correlation was observed between GGT and hsCRP concentration as well as both with HbA
1
c, FBS, and PP
2
BS.
Conclusions
Oxidative stress and inflammation appears to be a key component and also associated with poor glycemic control and further pathogenesis of diabetes and its complications. All our finding suggesting a link between oxidative stress, inflammation and glycemic control in patient with type 2 diabetes mellitus.
Abstract
Objective
The aim of this study was to see the effect of hypoproteinemia on electrolyte measurement by two different techniques, that is, direct ion selective electrode (ISE) and indirect ...ISE.
Material and Method
It was an observational study in which 90 serum samples with normal protein content (Group-1) were subjected to sodium (Na
+
) and potassium (K
+
) measurements by direct and indirect ISE methods. In the same way, 90 serum samples with total protein < 5 g/dL (Group-2) were subjected to Na
+
and K
+
measurements by direct and indirect ISE methods.
Result
In samples from Group-1 patients, average Na
+
was 138.1 ± 4.764 mmol/L by direct ISE method and 139.3 ± 3.887 mmol/L by indirect ISE method while average K
+
was 4.41 ± 0.644 mmol/L by direct ISE method and 4.40 ± 0.592 mmol/L by indirect ISE method. There was no statistically significant difference in Na
+
and K
+
values measured by different methods. In samples from Group-2 patients, measured value of Na
+
by direct ISE and indirect ISE was 134.57 ± 5.520 mmol/L and 138.64 ± 5.401 mmol/L, respectively. Difference between these two values was statistically significant with
p
-value of < 0.0001, but direct ISE and indirect ISE measured values of K
+
was 4.146 ± 0.9639 mmol/L and 4.186 ± 0.8989, respectively, with no significant difference.
Conclusion
Direct and indirect ISE methods are not comparable and showing significantly different results for Na
+
in case of hypoproteinemia. So, it is recommended that setups like intensive care unit or emergency department, where electrolyte values have significant treatment outcome, should follow direct ISE method and should compare its previous result with the same method. Both the methods should not be used interchangeably.
The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release.
Biodegradable in situ injectable implants were prepared by polymer ...precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed.
The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics.
Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.
The purpose of this research was to develop mouth dissolve tablets of nimesulide. Granules containing nimesulide, camphor, crospovidone, and lactose were prepared by wet granulation technique. ...Camphor was sublimed from the dried granules by exposure to vacuum. The porous granules were then compressed. Alternatively, tablets were first prepared and later exposed to vacuum. The tablets were evaluated for percentage friability, wetting time, and disintegration time. In the investigation, a 32 full factorial design was used to investigate the joint influence of 2 formulation variables: amount of camphor and crospovidone. The results of multiple linear regression analysis revealed that for obtaining a rapidly disintegrating dosage form, tablets should be prepared using an optimum concentration of camphor and a higher percentage of crospovidone. A contour plot is also presented to graphically represent the effect of the independent variables on the disintegration time and percentage friability. A checkpoint batch was also prepared to prove the validity of the evolved mathematical model. Sublimation of camphor from tablets resulted in superior tablets as compared with the tablets prepared from granules that were exposed to vacuum. The systematic formulation approach helped in understanding the effect of formulation processing variables.
Obesity and overweight have become a worldwide epidemic, and there is an urgent need to examine childhood obesity and overweight across countries using a standardized international standard. In the ...present study we have investigated the prevalence of obesity and overweight and their association with socioeconomic status (SES) and the risk factors like diet, physical activity like exercise, sports, sleeping habit in afternoon, eating habits like junk food, chocolate, eating outside at weekend, family history of diabetes and obesity.
The study was carried out in 5664 school children of 12-18 years of age and having different SES. The obesity and overweight were considered using an updated body mass index reference. SES and life style factors were determined using pre-tested questionnaire.
Age-adjusted prevalence of overweight was found to be 14.3% among boys and 9.2% among girls where as the prevalence of obesity was 2.9% in boys and 1.5% in girls. The prevalence of overweight among children was higher in middle SES as compared to high SES group in both boys and girls whereas the prevalence of obesity was higher in high SES group as compared to middle SES group. The prevalence of obesity as well as overweight in low SES group was the lowest as compared to other group. Eating habit like junk food, chocolate, eating outside at weekend and physical activity like exercise, sports, sleeping habit in afternoon having remarkable effect on prevalence on overweight and obesity among middle to high SES group. Family history of diabetes and obesity were also found to be positively associated.
Our data suggest that the prevalence of overweight and obesity varies remarkably with different socioeconomic development levels.
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