JOURNAL OF DRUG DELIVERY AND THERAPEUTICS

1-4

Authors: Xinwei Cheng

The application of nanomedicines has proved to be effective for the therapy of various types of cancer compared to conventional treatments such as chemotherapy and radiation therapy. The nanomedicines can treat various cancers with the precise target without affecting the normal cells. In addition, by utilizing of enhanced permeability and retention (EPR) effect, nanomedicines can selectively targeting disease site and yield very promising therapeutic results for cancer treatment. Among all available nanomedicines, organic materials such as polymers are widely used in recent decades as biomaterials for their favorable properties like excellent biocompatibility, easy design and preparation, several types of structures and interesting biomimetic character, which warrants the further evaluations on these kinds of innovative material. Inorganic nanoparticles such nanogold also demonstrated the ability to target cancer and can be employed as both therapeutic and imaging agents. This mini-review will give a brief discussion of using inorganic and organic nanoparticles for the treatment of cancer.

11-17

Authors: Saiprasanna Behera, Mrinmoy Gautam

The main objective of this study was to perform pharmacological evaluation of Stay-On Power Capsules in Rabbits (Non-Rodents) namely the aphrodisiac activity. The present investigation deals with Pharmacological Studies (Mating behaviour study, mating performance test, Hormonal analysis, Reproductive organ and spermal analysis) of Stay-On Power Capsules in Non-Rodents administered orally by gavage to Rabbits in accordance with the schedule Y of drugs and Cosmetic Act (2005). The acute toxicity study of Stay-On Power Capsules was done by up and down method. After the completion of acute toxicity studies, three different doses were selected for aphrodisiac activity such as 150, 300, and 600 mg/kg. Volume of oral administration was 1 ml/100 g of animals. Animals were randomly divided into five groups with six animals per group. Group I represented the control animals treated with normal water only; Groups II, III, and IV were treated with oral suspension of Stay-On Power Capsules at 18:00 h, at doses of 150, 300, and 600 mg/kg, respectively; and Group V served as a positive control treated with Sildenafil citrate of 5 mg/kg body weight. All the treatments were continued for 3 weeks only. A mating behaviour study revealed that continuous administration for 3 weeks, all the doses of Stay-On Power Capsules were able to significantly decrease mount and intromission latencies, and decrease ejaculatory latency and post ejaculatory interval when compared to vehicle control and standard drug treated Rabbits. It also resulted in a dose dependent increase in the mating performance and showed increasing ratio of testes body weight along with increase in sperm count as compared to the control group. Key Words: Stay-On Power Capsules, Pharmacological Studies, aphrodisiac activity, mating behaviour, mating performance

29-35

Authors: Awofisayo Sunday Olajide

The quality indices of dihydroartemisinin–piperaquine (DP) pediatric and adult (DPP and DPA) formulations of antimalarial were assessed. Moisture content, viscosity, total solid for four (DPP) products along with weight uniformity, tablet hardness, friability, disintegration and dissolution for six (DPA) products, were determined. Assay of chemical content was performed using reverse phase high pressure liquid chromatographic (RP-HPLC) with Zorbax Eclipse XDB C8 column (150 x 4.6 mm, 4.6 µm)), UV detection at 220 nm and flow rate of 0.7 mL/min. Acetonitrile: 10 mM ammonium acetate (70:30%, v/v) and tinidazole served as mobile phase and internal standard, respectively. Statistical analysis of data was performed using Minitab statistical software with one-way analysis of variance comparing the parameters among the formulations and confidence interval set at 95%. DPP products showed pH and moisture content within 3.19 to 4.65 units and 2.6 to 4.4%, respectively. Total solid and viscosity values were within 86.2 to 97.2% and 78.5 to 125.8 mPa.s, respectively. DPA products had comparable and satisfactory weight uniformity, hardness, friability and disintegration tests results except for DPA5 and DPA6 which failed the weight uniformity tests featuring tablets with deviation from the mean above 5%. All DPP products passed chemical content test with values within 92.65 to 101.22% while DPA2, DPA4 and DPA5 failed. All DPA products showed poor dissolution characteristics with C40 values below 60% and T70 values above 70 min. All DP products showed varying physicochemical properties that may give differing drug performance in vivo.

44-49

Authors: Birhanu Demeke Workneh, Terefe Teshome Kassa, Fantaye Teka Dinkashe, Tsegay Aregawi, Tigist Assefa Bayou, Meles Tekie Gidey, Yared Belete Belay

Introduction: Generic medicines are produced by multiple manufacturers hence, are usually cheaper than innovator brands and therefore save costs on medicines. Many physicians oppose brand substitution, believing generic medicines to be inferior to their originator counterparts. Physicians’ belief about generic medicines and factors affecting generic prescribing in Ethiopia are poorly investigated. Objective: To assess the physicians’ belief about generic medicines and to identify factors affecting generic medicines prescribing in private health facilities, Mekelle, Northern Ethiopia. Materials and Methods: An institution based cross-sectional study was conducted enrolling all physicians working in private health facilities. The data were collected from January 2016 to March 2016. Data were collected using self-administered structured questionnaires measuring generic medicines belief of physicians using a Likert scale of 1–5. Data were then entered into SPSS version 20 for analysis. Results: Of the fifty-six physicians approached in this study, 50 (89.2% response rate) questionnaires were included in the analysis. Nearly three-fourth (72%) of the physicians claimed that they always prescribe generic medicines. More than half (55.3) of the respondents beliefs generic medicines have different active ingredients than a brand innovator. Almost equal percentage (52% and 54%) of the Physicians disagreed with brand medicines were safer than generic medicines and prescribing generic due to the complicated health problem of the patient respectively. Around two third (67.5%) of physicians reported that quality profile of medicine was a major reason for prescribing generic medicines. Moreover, availability of medicines in pharmacies and low cost of medicines were the main reasons for prescribing generic medicines with 58.1% and 52.4% respectively. Conclusion: The majority of physicians do not have a positive perception of generic medicines and a significant portion of the physician’s belief brand medicines safer and effective than generic counterparts. The availability of medicines in pharmacies, low cost of medicines and purchasing power of the patients are major factors affecting generic medicines prescribing.

58-61

Authors: Mohammad Mujahid, Latif Ahmad, Mohammad Ahmad

Zinc oxide (ZnO) nanogel is an antimicrobial gel comprising of ZnO nanoparticles. Since, in nanoparticles, the surface to volume ratio is very large, therefore, ZnO nanogel is more effective for the treatment of superficial skin microbial infections as compared to other gels comprising ZnO and that has processed through traditional methods. Generally, infected skins are affected by bacterial strains which are attached to the surface of the skin by forming biofilms. The cause of attachment of these biofilms with the skin may be due to the electrostatic, van der walls, dipole-dipole and H-bonding hydrophobic types of interactions. ZnO nanogel when applied to the microbial infected skin reduces the microbial adhesion and biofilm formation. This screening characteristic of gel is due to the presence of ZnO nanoparticles of pore diameter 12.4 nm in the gel. The nanoparticles of ZnO is synthesized using sol-gel method and characterized by X - ray diffraction (XRD), field emission scanning electron microscopy (FESEM), energy dispersive spectroscopy (EDS) and high resolution transmission scanning electron microscopy (HRTEM). The minimum inhibitory concentration (MIC) data tells that ZnO nanoparticles of such a small pore diameter inhibit the growth of microbes present on the skin surface.

77-80

Authors: Devesh Kapoor

Extended release formulations are becoming more popular day by day for the delivery of non-steroidal anti-inflammatory drugs (NSAIDs) because of their ability to maintain optimal and therapeutically effective drug levels for prolonged duration with the reduction in dosing frequency and side effects associated with NSAIDs. Etodolac is a nonsteroidal anti-inflammatory drug. it is an inhibitor of cycloxygenase which belongs to the pyranocarboxylic acid group, which is effective in treating fever, pain, and inflammation in the body, which is degraded in the stomach. In the present study, a suitable particulate system of Etodolac has been developed, by ionotropic gelation method for sustained release that would result in prolonged clinical efficacy, reduced frequency of administration and lesser side effects. Microbeads were fabricated with and without using guar gum as polymer and were characterized for particle size and size distribution analysis, flow properties, loose surface crystal study, entrapment efficiency, swelling ratio, percentage yield and drug content uniformity and in-vitro drug release. It was found that the particle size distribution of both formulations was varied within a narrow size range. Drug leaching (14.98 % ± 0.118) was more with the presence of guar gum. Entrapment efficiency was retarded with the presence of guar gum. Swelling ratio (53.49 ± 1.874) advocated that guar gum incorporated microbeads swelled more to behave as a matrix for controlled drug delivery. Establishment of highly viscous dispersion with the incorporation of polymer led to high percentage yield (49.35% ± 01.230). Drug release data was fitted to various kinetic models and indicated that the mechanism was according to peppas model. The study discovered that the microbeads of Etodolac could be efficaciously formulated by ionotropic gelation technique with sustained release characteristics.

85-95

Authors: Hameed M Shahul, R K Jat, V N Indulatha

Objectives of this research work were development and validation of HPLC methods of analysis for Bosentan in tablet dosage form from single components as per the current ICH & USP guidelines. HPLC methods also validated for the marketed Bosentan from single components. This developed procedure applied for regular analysis of these medicaments in pharmaceutical industry The major scope of research is development of simple, accurate, reproducible & fast cost effective methods for new cefalosporins. The methods are validated with recovery studies using bulk drug of 80%, 120% & 40%. Specific method is confirmed by checkingdinterference of expients & assay method. The interday & intraday assay are also performed for checking robustness of the system. The minimum detection limit is checked by using formula LOD = 3.3 sigma (St&nd deviation) / Slop, where σ indicate st&ard deviation & S denotes slop of the regression straight line. The wuantification limit is detrmined by using LOQ = 10 σ d(St&. dev.)/ S that is minimum concentration of drug can be quantified. Linearity is found in the limit of Beer’s law, straight line was constructed within the given range of the conc. of the drugs. So can develop & validate a new, reproducible, correct, & easy, less time consuming, cheap & ecofriendly method for daily analysis of drug in our general life.

99-101

Authors: Alla Seetha Devi, Kasi R Rao, B Nagamani, Ramana Ch Reddy, Venkata P Krishna

Paracetamol (acetaminophen) with caffeine is a combination medicine indicated for the temporary relief of pain and discomfort associated with a number of conditions such as headache or muscle pain. Paracetamol has a narrow safety margin and there are number of risks associated with paracetamol. It is only safe and effective when used according to directions on OTC (Over- The-Counter) and Rx labelling. However, long-term use of paracetamol increases the risk of kidney and liver failure and makes people more vulnerable to high blood pressure and strokes. Chronic or excessive administration of caffeine has been implicated in a range of dysfunctions involving the liver, renal system, gastrointestinal system, and musculature. A patient taking the combination of paracetamol with caffeine may be more likely to experience adverse effects than to get improved analgesia, compared with paracetamol alone.

110-118

Authors: Yalew Molla, Mekonnen Sisay

Most of the physiological effects of the rennin-angiotensin system (RAS) are mediated by angiotensin II (AgII) type one receptors (AT1R), producing cellular dedifferentiation and proliferation; vasoconstriction; renal tubule sodium (Na+) reabsorption etc. However, the pathophysiologic role of AgII type two receptor (AT2R) has not been clearly defined yet. This review was, therefore, aimed at summarizing a plenty of primary literatures related to the role of AT2R. AT2R is a special G protein coupled receptor that is not coupled with the usual second messengers. The expression level of AT2R is greater in the neonates and fetal ages than in adults though its expression is up-regulated following tissue injury in adults implicating its role in regulating cell differentiation, growth and inflammations. Most of the cellular actions mediated by AT2R are counter regulatory to that of AT1R. AgII produces the cellular effects by acting on AT2R via different signal transduction pathways. The common cellular effects mediated by AT2R are antiproliferative, anti-inflammatory, vasodilation, natriuresis, etc which may be essential for modulating the cardiovascular, renal and brain injuries caused by different etiologies. The principal molecular signal transductions mediated by AT2R involve stimulation of the bradykinin and/or nitric oxide-cGMP pathwy, inactivation of mitogen activated protein kinase pathway by stimulating tyrosine and serine/threonien phosphatses, production of the neuroprotective factors, like BDNF, etc. These signaling pathways may exert cardio-renal and neuroprotective functions. Therefore, the development of drugs that stimulate the AT2R may the potential target to promote the treatment of different disorders related to the cardiovascular, renal and brain dysfunctions.

128-131

Authors: Merin Mathew, K Krishnakumar, B Dineshkumar, Smitha K Nair

Nanosuspensions are colloidal dispersions and biphasic system consisting of drug particles dispersed in an aqueous vehicle in which the diameter of the suspended particle is less than 1μm in size. Many drugs including antibiotics are having poor solubility. Nanosuspensions have proven to be a better alternative over other approaches currently available for improving bioavailability of such drugs with low solubility. This review describes the methods of pharmaceutical nanosuspension of antibiotic formulations and pharmaceutical applications in drug delivery.