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   2011| January-March  | Volume 3 | Issue 1  
    Online since February 5, 2011

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Mucoadhesive drug delivery systems
Rahamatullah Shaikh, Thakur Raghu Raj Singh, Martin James Garland, A David Woolfson, Ryan F Donnelly
January-March 2011, 3(1):89-100
DOI:10.4103/0975-7406.76478  PMID:21430958
Mucoadhesion is commonly defined as the adhesion between two materials, at least one of which is a mucosal surface. Over the past few decades, mucosal drug delivery has received a great deal of attention. Mucoadhesive dosage forms may be designed to enable prolonged retention at the site of application, providing a controlled rate of drug release for improved therapeutic outcome. Application of dosage forms to mucosal surfaces may be of benefit to drug molecules not amenable to the oral route, such as those that undergo acid degradation or extensive first-pass metabolism. The mucoadhesive ability of a dosage form is dependent upon a variety of factors, including the nature of the mucosal tissue and the physicochemical properties of the polymeric formulation. This review article aims to provide an overview of the various aspects of mucoadhesion, mucoadhesive materials, factors affecting mucoadhesion, evaluating methods, and finally various mucoadhesive drug delivery systems (buccal, nasal, ocular, gastro, vaginal, and rectal).
  37,278 1,632 199
Differential scanning calorimetry: An invaluable tool for a detailed thermodynamic characterization of macromolecules and their interactions
Michael H Chiu, Elmar J Prenner
January-March 2011, 3(1):39-59
DOI:10.4103/0975-7406.76463  PMID:21430954
Differential Scanning Calorimetry (DSC) is a highly sensitive technique to study the thermotropic properties of many different biological macromolecules and extracts. Since its early development, DSC has been applied to the pharmaceutical field with excipient studies and DNA drugs. In recent times, more attention has been applied to lipid-based drug delivery systems and drug interactions with biomimetic membranes. Highly reproducible phase transitions have been used to determine values, such as, the type of binding interaction, purity, stability, and release from a drug delivery mechanism. This review focuses on the use of DSC for biochemical and pharmaceutical applications.
  24,341 796 144
Acute-phase proteins: As diagnostic tool
Sachin Jain, Vidhi Gautam, Sania Naseem
January-March 2011, 3(1):118-127
DOI:10.4103/0975-7406.76489  PMID:21430962
The varied reactions of the host to infection, inflammation, or trauma are collectively known as the acute-phase response and encompass a wide range of pathophysiological responses such as pyrexia, leukocytosis, hormone alterations, and muscle protein depletion combining to minimize tissue damage while enhancing the repair process. The mechanism for stimulation of hepatic production of acute-phase proteins is by proinflammatory cytokines. The functions of positive acute-phase proteins (APP) are regarded as important in optimization and trapping of microorganism and their products, in activating the complement system, in binding cellular remnants like nuclear fractions, in neutralizing enzymes, scavenging free hemoglobin and radicals, and in modulating the host's immune response. APP can be used as diagnostic tool in many diseases like bovine respiratory syncytial virus, prostate cancer, bronchopneumonia, multiple myeloma, mastitis, Streptococcus suis infection, starvation, or lymphatic neoplasia. Thus, acute-phase proteins may provide an alternative means of monitoring animal health.
  15,550 668 171
A review on phytochemical and pharmacological investigations of miswak (Salvadora persica Linn)
Jamal Akhtar, Khalid M Siddique, Salma Bi, Mohd Mujeeb
January-March 2011, 3(1):113-117
DOI:10.4103/0975-7406.76488  PMID:21430961
The miswak is a natural toothbrush made from the twigs of the Salvadora persica (Salvadoraceae). Its use predates the inception of Islam and is frequently advocated in the Hadith (the traditions relating to the life of Prophet Muhammad PBUH ). In addition to strengthening the gums, it prevents tooth decay, eliminating toothaches and halt further increase in decay that has already set in. It creates a fragrance in the mouth, eliminates bad odor, improves the sense of taste, and causes the teeth to glow and shine. The other parts of the tree have therapeutic values as corrective, deobstruent, liver tonic, diuretic, analgesic, anthelmintic, astringent, lithontriptic, carminative, diuretic, aphrodisiac, and stomachic. The present review is therefore an effort to give detailed survey of the literature on phytochemistry and pharmacological activities of miswak.
  14,369 356 27
The thermodynamics of simple biomembrane mimetic systems
Antonio Raudino, Maria Grazia Sarpietro, Martina Pannuzzo
January-March 2011, 3(1):15-38
DOI:10.4103/0975-7406.76462  PMID:21430953
Insight into the forces governing a system is essential for understanding its behavior and function. Thermodynamic investigations provide a wealth of information that is not, or is hardly, available from other methods. This article reviews thermodynamic approaches and assays to measure collective properties such as heat adsorption / emission and volume variations. These methods can be successfully applied to the study of lipid vesicles (liposomes) and biological membranes. With respect to instrumentation, differential scanning calorimetry, pressure perturbation calorimetry, isothermal titration calorimetry, dilatometry, and acoustic techniques aimed at measuring the isothermal and adiabatic processes, two- and three-dimensional compressibilities are considered. Applications of these techniques to lipid systems include the measurement of different thermodynamic parameters and a detailed characterization of thermotropic, barotropic, and lyotropic phase behavior. The membrane binding and / or partitioning of solutes (proteins, peptides, drugs, surfactants, ions, etc.) can also be quantified and modeled. Many thermodynamic assays are available for studying the effect of proteins and other additives on membranes, characterizing non-ideal mixing, domain formation, bilayer stability, curvature strain, permeability, solubilization, and fusion. Studies of membrane proteins in lipid environments elucidate lipid-protein interactions in membranes. Finally, a plethora of relaxation phenomena toward equilibrium thermodynamic structures can be also investigated. The systems are described in terms of enthalpic and entropic forces, equilibrium constants, heat capacities, partial volume changes, volume and area compressibility, and so on, also shedding light on the stability of the structures and the molecular origin and mechanism of the structural changes.
  12,692 146 4
Biomembrane models and drug-biomembrane interaction studies: Involvement in drug design and development
R Pignatello, T Musumeci, L Basile, C Carbone, G Puglisi
January-March 2011, 3(1):4-14
DOI:10.4103/0975-7406.76461  PMID:21430952
Contact with many different biological membranes goes along the destiny of a drug after its systemic administration. From the circulating macrophage cells to the vessel endothelium, to more complex absorption barriers, the interaction of a biomolecule with these membranes largely affects its rate and time of biodistribution in the body and at the target sites. Therefore, investigating the phenomena occurring on the cell membranes, as well as their different interaction with drugs in the physiological or pathological conditions, is important to exploit the molecular basis of many diseases and to identify new potential therapeutic strategies. Of course, the complexity of the structure and functions of biological and cell membranes, has pushed researchers toward the proposition and validation of simpler two- and three-dimensional membrane models, whose utility and drawbacks will be discussed. This review also describes the analytical methods used to look at the interactions among bioactive compounds with biological membrane models, with a particular accent on the calorimetric techniques. These studies can be considered as a powerful tool for medicinal chemistry and pharmaceutical technology, in the steps of designing new drugs and optimizing the activity and safety profile of compounds already used in the therapy.
  11,668 210 69
Importance of phenols structure on their activity as antinitrosating agents: A kinetic study
Marcia Pessego, Ana M Rosa da Costa, Jose A Moreira
January-March 2011, 3(1):128-134
DOI:10.4103/0975-7406.76491  PMID:21430963
Objective : Nitrosative deamination of DNA bases induced by reaction with reactive nitrogen species (RNS) has been pointed out as a probable cause of mutagenesis. (Poly)phenols, present in many food items from the Mediterranean diet, are believed to possess antinitrosating properties due to their RNS scavenging ability, which seems to be related to their structure. It has been suggested that phenolic compounds will react with the above-mentioned species more rapidly than most amino compounds, thus preventing direct nitrosation of the DNA bases and their transnitrosation from endogenous N-nitroso compounds, or most likely from the transient N-nitrosocompounds formed in vivo. Materials and Methods : In order to prove that assumption, a kinetic study of the nitroso group transfer from a N-methyl-N-nitrosobenzenesulfonamide (N-methyl-N-nitroso-4-methylbenzenesulfonamide, MeNMBS) to the DNA bases bearing an amine group and to a series of phenols was carried out. In the transnitrosation of phenols, the formation of nitrosophenol was monitored by Ultraviolet (UV) / Visible spectroscopy, and in the reactions of the DNA bases, the consumption of MeNMBS was followed by high performance liquid chromatography (HPLC). Results : The results obtained point to the transnitrosation of DNA bases being negligible, as well as that of phenols bearing electron-withdrawing groups. Phenols with methoxy substituents in positions 2, 4, and / or 6, although they seemed to react, did not afford the expected product. Phenols with electron-releasing substituents, unless these blocked the oxygen atom, reacted with our model compound at an appreciable rate. O-nitrosation of the phenolate ion followed by rearrangement of the C-nitrosophenol seemed to be involved. Conclusion : This study provided evidence that the above compounds might actually act as antinitrosating agents in vivo.
  7,923 82 7
Biofunctional prosthetic system: A new era complete denture
Vandana Saini, Ruchi Singla
January-March 2011, 3(1):170-172
DOI:10.4103/0975-7406.76505  PMID:21430970
  6,183 403 -
Generic antibiotic industries: Challenges and implied strategies with regulatory perspectives
M Venkatesh, VG Bairavi, KC Sasikumar
January-March 2011, 3(1):101-108
DOI:10.4103/0975-7406.76481  PMID:21430959
Ever since the discovery of antibiotics, the quality of human life greatly improved in the 20 th century. The discovery of penicillin transformed the medicine industry and initiated a search for a better antibiotic every time resulting in several synthetic and semi-synthetic antibiotics. Beginning with the 1937 sulfa drug tragedy, the drug regulations had a parallel growth along with the antibiotics and the antibiotic-based generic Pharma industries. This review article is focused on the scenario depicting current global Pharma industries based on generic antibiotics. Several regulatory aspects involved with these industries have been discussed along with the complexity of the market, issues that could affect their growth, their struggle for quality, and their compliance with the tightened regulations. With the skyrocketing commercialization of antibiotics through generics and the leveraging technologic renaissance, generic industries are involved in providing maximum safer benefits for the welfare of the people, highlighting its need today.
  5,592 149 7
Highly active antiretroviral therapy: Does it Sound toxic?
Katijah Khoza-Shangase
January-March 2011, 3(1):142-153
DOI:10.4103/0975-7406.76494  PMID:21430965
Objective : The main objective of the current study is to monitor the auditory status in a group of adults with AIDS, receiving Highly Active Antiretroviral Therapy (HAART) (3TC -lamivudine, D4T - stavudine, and efavirenz) in a hospital outpatient clinic in Gauteng. A total sample of 54 adults (between the ages of 18 and 50 years) in the experimental group and 16 in the control group were assessed prospectively following a repeated measures design. All participants were assessed at baseline at three months, and at six months into the treatment. Materials and Methods : The participants underwent case history interviews and medical record reviews, otoscopy, and tympanometry, as well as conventional pure tone audiometry and distortion product otoacoustic emission testing. Both descriptive and inferential statistics were used to analyze the data. Results : On audiological monitoring, statistically significant changes (P<0.05) were established, only in the experimental group, for pure tone audiometry - with clinically significant changes found at high frequencies. Statistically significant changes with clinically significant changes were obtained for distortion product otoacoustic emissions (DPOAEs) in the experimental group, particularly at high frequencies - implying subclinical hearing function changes; while lack of statistically significant changes with no clinically significant changes were found in the control group. The subclinical hearing changes in the experimental group were also evident in the findings of the subclinical hearing loss group, who, although they had normal pure tone function after six months of follow up, presented with clinical changes on DPOAEs at 6 and 8 kHz. Conclusions : Findings highlight the need for closer monitoring of the effects of antiretroviral drugs (ARVs) on hearing, through the use of more sensitive tools of assessment when conducting drug trials.
  4,443 92 14
Effect of solar eclipse on microbes
Amrita Shriyan, Angri M Bhat, Narendra Nayak
January-March 2011, 3(1):154-157
DOI:10.4103/0975-7406.76498  PMID:21430966
Objective : A solar eclipse was observed in India on 15 th January, 2010. It was a total eclipse in some parts of the country, while it was a partial eclipse in other parts. Microorganisms play an important role in various phenomena on the earth. This study was undertaken to know the influence of solar eclipse on nature indirectly, by analyzing certain genotypic and phenotypic variations in prokaryotes and eukaryotes. Since yeast have similar gene expression as that of humans, investigations were pursued on Candida albicans. Hence the study of the effect of solar eclipse on cultures of Staphylococcus aureus, Klebsiella species, Escherichia coli, and C. albicans was performed in the laboratory. The effect of the total or partial eclipse on the microorganism isolated from clinical isolates was investigated during the time period from 11.15 am to 3.15 pm. Materials and Methods : Cultures of S. aureus, Klebsiella species, and E. coli colonies on nutrient agar slants and broth and C. albicans on Sabouraud's dextrose agar plates and broth. Slants were exposed to sunlight during eclipse and exposure to normal sunlight at Mangalore, Dakshina Kannada district, Karnataka state, India. Results : There was significant change observed during exposure to normal sunlight and eclipse phase. Bacterial colonies showed difference in morphology on smear examination and sensitivity pattern during this study. One fungal species and three bacterial isolates were studied and changes were recorded. Fungal species showed a definite change in their morphology on exposure to sunlight during eclipse observed by stained smear examination from broth, plate, and slant. Conclusion : Present study concludes that blocking of the sun rays during eclipse does not harm prokaryotes and eukaryotes, instead promoted the progeny of predators in the race of better acclimatization and survival in the natural and changing environmental conditions.
  4,132 97 1
Nucleic acid-lipid membrane interactions studied by DSC
Sarantis Giatrellis, George Nounesis
January-March 2011, 3(1):70-76
DOI:10.4103/0975-7406.76470  PMID:21430956
The interactions of nucleic acids with lipid membranes are of great importance for biological mechanisms as well as for biotechnological applications in gene delivery and drug carriers. The optimization of liposomal vectors for clinical use is absolutely dependent upon the formation mechanisms, the morphology, and the molecular organization of the lipoplexes, that is, the complexes of lipid membranes with DNA. Differential scanning calorimetry (DSC) has emerged as an efficient and relatively easy-to-operate experimental technique that can straightforwardly provide data related to the thermodynamics and the kinetics of the DNA-lipid complexation and especially to the lipid organization and phase transitions within the membrane. In this review, we summarize DSC studies considering nucleic acid-membrane systems, accentuating DSC capabilities, and data analysis. Published work involving cationic, anionic, and zwitterionic lipids as well as lipid mixtures interacting with RNA and DNA of different sizes and conformations are included. It is shown that despite limitations, issues such as DNA- or RNA-induced phase separation and microdomain lipid segregation, liposomal aggregation and fusion, alterations of the lipid long-range molecular order, as well as membrane-induced structural changes of the nucleic acids can be efficiently treated by systematic high-sensitivity DSC studies.
  3,930 85 10
Genetic screening: The vista of genomic medicine
Rajiv Saini, Santosh Saini, Gagan Saini
January-March 2011, 3(1):109-112
DOI:10.4103/0975-7406.76487  PMID:21430960
The accelerating development of biochemical and DNA-based diagnostic tests for human genetic conditions in the last decade has engendered a revolution in genetic diagnosis. Both genetic testing and genetic screening involve the same testing processes to examine an individual's chromosomes, DNA, or the biochemical product of a gene, typically a protein to confirm or refute a suspected chromosomal, DNA, or gene product change. The identification of genetic disorders, and the potential for developing a therapy, is a powerful force in genetics and medicine.
  3,832 75 -
Transfer kinetics from colloidal drug carriers and liposomes to biomembrane models: DSC studies
Maria Grazia Sarpietro, Francesco Castelli
January-March 2011, 3(1):77-88
DOI:10.4103/0975-7406.76472  PMID:21430957
The release of bioactive molecules by different delivery systems has been studied. We have proposed a protocol that takes into account a system that is able to carry out the uptake of a bioactive molecule released during the time, resembling an in vivo-like system, and for this reason we have used biomembrane models represented by multi-lamellar and unilamellar vesicles. The bioactive molecule loaded delivery system has been put in contact with the biomembrane model and the release has been evaluated, to consider the effect of the bioactive molecule on the biomembrane model thermotropic behavior, and to compare the results with those obtained when a pure drug interacts with the biomembrane model. The differential scanning calorimetry technique has been employed. Depending on the delivery system used, our research permits to evaluate the effect of different parameters on the bioactive molecule release, such as pH, drug loading degree, delivery system swelling, crosslinking agent, degree of cross-linking, and delivery system side chains.
  3,610 83 6
The influence of epidural anesthesia on new-born hearing screening: A pilot study
Katijah Khoza-Shangase, Karin Joubert
January-March 2011, 3(1):135-141
DOI:10.4103/0975-7406.76493  PMID:21430964
Objective : The main aim was to establish if epidural anesthesia had an influence on new-born hearing screening results in newborns born via elective Cesarean section in healthy pregnancies. Specific objectives included determining screening results in a group of newborns born to mothers who had undergone epidural anesthesia during Cesarean section childbirth (experimental group); and comparing the findings with those of a group of newborns born to mothers who had undergone natural delivery without epidural anesthesia (comparison group); while establishing if the time of screening following delivery had any effect on the overall screening results. Materials and Methods : The above objectives were achieved through the use of a prospective quasi-experimental repeated measures design with a comparison group, where 40 newborns (20 in the experimental and 20 in the comparison group) were screened at three different times through transient otoacoustic emissions (TEOAEs) and automated auditory brainstem response (AABR) measures. All participants were screened while resting quietly in open bassinets in an empty new-born nursery. For both test measures, the results were recorded as either pass or refer. Data were analyzed through both descriptive and inferential statistics. Results : Findings indicated that hearing screening earlier than four hours after birth, for both the experimental and comparison groups yielded more false positive findings than testing conducted after 24 hours. An index of suspicion in relation to the influence of epidural anesthesia on Automated Auditory Brainstem Response (AABR), when conducted less than four hours after birth, was raised, as statistically significant findings (P<0.05) were obtained. Conclusions : The findings have implications for timing of screening where universal newborn hearing screening is being implemented.
  3,636 55 9
A survey: Precepts and practices in drug use indicators at government healthcare facilities: A hospital-based prospective analysis
Hettihewa L Menik, Amrasinghe I Isuru, Subasinghe Sewwandi
January-March 2011, 3(1):165-169
DOI:10.4103/0975-7406.76502  PMID:21430968
Background : We planned to identify the difficulties in practicing the rational use of medicine in health facilities, using drug-use indicators. Materials and Methods : We studied the average consultation time (ACT), average number of drugs per encounter (ANDE), percentage of drugs by generic name (PDPG), percentage of encounters with antibiotics (PAP), percentage of encounters with injection (PIP), percentage of drugs prescribed from the essential drugs list (PEDL), using pretested questionnaires in different hospital types. Results : There was a higher value of ACT in Teachin hospital (TH,2.31 min) and general hospital (GH,2.17 min) compared to district hospital (DH ,0.83 min). ANDE was high in all three categories (3.24, 2.88, and 3.26 in TH, GH, and DH, respectively). There was a significant difference in ANDE in all three categories ( P≤0.05). There was no significant difference in the PDPG among all categories of Hospitals. PAP was highest in DH (80%) and lowest in GH (46%). PIP was highest in DH (6%), 4% in GH, and lowest in TH (3%) in the Galle district. PEDL in TH, GH, and DH were 97, 100, and 99%, respectively. Prescribers use a short consultation time and practice polypharmacy, and the use of generic and essential drug lists is significantly high. Antibiotic usage is high, but usage of injections is low. We further noted prescriptions with absence of the diagnosis, sex, and prescriber's identity. Conclusion : We conclude that some areas like polypharmacy, high usage of antibiotics, and poor prescription writing practices are high and they can be addressed by in-service awareness programs for noted prescriber errors.
  3,383 114 5
Clinical efficacy and health implications of inconsistency in different production batches of antimycotic drugs in a developing country
Adenike A.O Ogunshe, Adedayo A Adepoju, Modupe E Oladimeji
January-March 2011, 3(1):158-164
DOI:10.4103/0975-7406.76501  PMID:21430967
Objective : This study aimed at evaluating the in vitro efficacy and health implications of inconsistencies in different production batches of antimycotic drugs. Materials and Methods : In vitro susceptibility profiles of 36 Candida spp. - C. albicans (19.4%), C. glabrata (30.6%), C. tropicalis (33.3%), and C. pseudotropicalis (16.7%) - obtained from human endocervical and high vaginal swabs (ECS/HVS) to two different batches (B1 and B2) of six antimycotic drugs (clotrimazole, doxycycline, iconazole, itraconazole, metronidazole and nystatin) was determined using modified agar well-diffusion method. Results : None of the Candida strains had entirely the same (100%) susceptibility / resistance profiles in both batches of corresponding antimycotic drugs; while, different multiple antifungal susceptibility (MAS) rates were also recorded in batches 1 and 2 for corresponding antifungals. Only 14.3%, 27.3%, 16.7-33.3%, and 8.3-25.0% of C. albicans, C. glabrata, C. pseudotropicalis, and C. tropicalis strains, respectively, had similar susceptibility/resistance profiles toward coressponding antifungal agents in both batches; while up to 57.1% of C. albicans, 45.5% of C. glabrata, 66.7% of C. pseudotropicalis, and 50.0% of C. tropicalis strains were susceptible to one batch of antifungals but resistant to corresponding antifungals in the second batch. As high as 71.4% (C. albicans), 73.0% (C. glabrata), 50.0% (C. pseudotropicalis), and 66.74% (C. tropicalis) strains had differences of ≥10.0 mm among corresponding antimycotic agents. Conclusions : Candida strains exhibited different in vitro susceptibility / resistance patterns toward two batches of corresponding antimycotic agents, which has clinical implications on the efficacy of the drugs and treatment of patients. The findings of the present study will be of benefit in providing additional information in support of submission of drugs for registration to appropriate regulatory agencies.
  3,376 61 1
Calorimetric techniques to study the interaction of drugs with biomembrane models
Rosario Pignatello, Francesco Castelli
January-March 2011, 3(1):1-2
DOI:10.4103/0975-7406.76459  PMID:21430950
  3,035 113 2
Launch of the special issue of JPBS on CBRN disaster management
Himanshu Gupta
January-March 2011, 3(1):3-3
DOI:10.4103/0975-7406.76460  PMID:21430951
  2,653 118 -
C- and N-truncated antimicrobial peptides from LFampin 265 - 284: Biophysical versus microbiology results
Regina Adão, Kamran Nazmi, Jan G.M. Bolscher, Margarida Bastos
January-March 2011, 3(1):60-69
DOI:10.4103/0975-7406.76467  PMID:21430955
Lactoferrin is a glycoprotein with two globular lobes, each having two domains. Since the discovery of its antimicrobial properties, efforts have been made to find peptides derived from this protein showing antimicrobial properties. Most peptides initially studied were derived from Lactoferricin B, obtained from the protein by digestion with pepsin. More recently, a new family of antimicrobial peptides (AMPs) derived from Lactoferrin was discovered by Bolcher et al, and named Lactoferrampin (LFampin). The original sequence of LFampin contained residues 268 - 284 from the N1 domain of Lactoferrin. From this peptide, the Bolscher's group synthesized a collection of peptides obtained by extension and / or truncation at the C or N-terminal sides, in order to unravel the main structural features responsible for antimicrobial action. Here, we present results for three of these peptides, namely LFampin 265 - 284, LFampin 265 - 280, and LFampin 270 - 284. The peptides were tested against bacteria (E. coli and S. sanguinis), fungi (C. albicans), and model membranes of 1,2-dimyristoyl-sn-glycero-3-phosphocholine (DMPC), 1,2-dimyristoyl-sn-glycero-3-[phospho-rac-(1-glycerol)] (DMPG), and their mixtures at a ratio of 3 : 1 (DMPC : DMPG (3 : 1)). The ability to adopt a helical conformation was followed by a circular dichroism (CD), and the perturbation of the gel to the liquid-crystalline phase transition of the membrane was characterized by differential scanning calorimetry (DSC). Distinct behavior was observed in the three peptides, both from the microbiology and model membrane studies, with the biophysical results showing excellent correlation with the microbiology activity studies. LFampin 265 - 284 was the most active peptide toward the tested microorganisms, and in the biophysical studies it showed the highest ability to form an a-helix and the strongest interaction with model membranes, followed by LFampin 265 - 280. LFampin 270 - 284 was inactive, showing marginal secondary structure and no interaction with the pathogen model membranes.
  2,717 53 20
Vitamins and periodontitis
Rajiv Saini
January-March 2011, 3(1):170-170
DOI:10.4103/0975-7406.76503  PMID:21430970
  2,147 100 1