JOURNAL OF DRUG DELIVERY AND THERAPEUTICS

4-16

Authors: Tanvi Rajput, Meenakshi K Chauhan

The human body has long provided pharmaceutical science with biomaterials of interesting applications. Bile salts (BSs) are biomaterials reminiscent of traditional surfactants with peculiar structure and self-assembled topologies. Most of the new drugs, biological therapeutics (proteins/peptides) and vaccines have poor performance after oral administration due to poor solubility or degradation in the gastrointestinal tract (GIT). Though, vesicular carriers exemplified by liposomes or niosomes can protect the entrapped agent to a certain extent from degradation. Nevertheless, the harsh GIT environment i.e, low pH, the presence of bile salts and enzymes limits their capabilities by destabilizing them. In response to that, more resistant bile salts-containing vesicles (BS-vesicles) were developed by the inclusion of bile salts into lipid bilayers constructs. Tremendous research in the last decade has made bilosomes a potential carrier system. Bilosomes with its name derived from bile salts (which is one of its major constituents), is a ‘niosome-like’ colloidal carrier. Here, we focus on different aspects of bile salt based drug delivery systems including their composition, developmental techniques, characterization, comparative advantages of BS-integrated nanomedicines over conventional nanocarriers, stability, transitional modifications and scale-up – emphasizing their biomedical potential in oral immunization against various diseases and delivery of peptide drugs. Bile acid-based amphiphiles, in the form of mixed micelles, bilosomes, drug conjugates and hybrid lipid-polymer nanoparticles are critically discussed as delivery systems for anticancer drugs, antimicrobial agents and therapeutic peptides/proteins, including vaccines. Current pitfalls, future perspectives, and opinions have also been outlined. Bile acid-based nanoparticles are a growing research area therefore, multifaceted pharmaceutical and biomedical applications of bile salts are to be expected in the near future.

22-26

Authors: Taranjit Kaur, Prachi Sharma, Sandeep Kumar

Certain techniques are used for the preparation of solid dispersions and used to enhance the solubility of water insoluble drugs. One of its techniques is supercritical fluid technology that is used for the preparation of solid dispersions. The present aim of this technique is to provide the recent advances in the use of supercritical fluids for the preparation of solid dispersion and for pharmaceutical substances with particular attention to drug delivery systems. Basically, a “supercritical fluid” can be defined as it enters in the pure substance when both temp. & pressure above its critical P&T. In the SCF techniques, there are certain solvents like CO2, N2O used as the supercritical fluid. This innovative technique is highly promising and approachable for the future applications in pharmaceutical industries.

33-41

Authors: Venkatesh D Nagasamy, Arun R, S. Saraswathi, MS Padma Priya, N Imran Khan, N Kathirulla, S Sruthi

Diacerein is generally used in the treatment of Osteoarthritis , this drug comes under the class anthraquinone. The drug is practically insoluble in water and exhibits exceptionally slow and intrinsic dissolution rate with poor bioavailability. In the present study, diacerein and β-cyclodextrin (β-CD) solid dispersions were prepared with a view to study the effect and influence of β-CD on the solubility and dissolution rate of this poorly aqueous soluble drug. Phase solubility profile revealed that the solubility of diacerein was significantly increased in the presence of β-CD and indicating the possible 1:1 stoichiometric inclusion complex with a stability constant of 339.66 M-1. Effect of variable such as drug: Carrier ratios were studied. Physical characterization of the solid dispersion was characterized by Fourier transform infrared spectroscopy (FT-IR), Differential scanning calorimetry (DSC) and X-ray diffraction studies (XRD). These studies revealed that a distinct loss of drug crystallinity in the solid dispersion is ostensibly accounting for enhancement of dissolution rate in distilled water containing 0.1% Tween 80. The scanning electron microscopy (SEM) study revealed that all the binary systems appeared as agglomerates and exhibiting the presence of a homogenous solid phase which could also be responsible for the enhanced dissolution rate in comparison with the pure drug. The drug release from the prepared solid dispersion exhibited a first order kinetics. Solid dispersion of diacerein showed a 7.66 times fold increase in dissolution rate over the pure drug.

53-60

Authors: Kamou Richard KAMOU, Yessé Zinzendorf NANGA, Abou OUATTARA, Sansan Philippe KAMBOU, Gouéh GNAHOUE, Calixte BAHI, Adama COULIBALY

This preliminary work consists in evaluating the superficial anticandidic activity of the leaves of Combretum racemosum P. Beauv in humans. To this end, we first demonstrated bioactive compounds of five (5) crude extracts (aqueous and hydro-organic 70%) from C. racemosum. Then, and finally, we have separately evaluated the superficial anticandidic activity of these extracts on Candida albicans, a species of genus Candida, mostly encountered in superficial human candidiasis. C. albicans was found to be sensitive to the five extracts tested. This partly justifies the use of C. racemosum in traditional medical practice against superficial microbial diseases. For these extracts, the Inhibitory Minimum Concentrations (MIC) recorded ranged from 7.8125 mg/mL to 62.550 mg/mL; While Fungicide Minimum Concentrations (CMF) range from 31.25 ± 0.00 mg/mL to 62.550 mg/mL. Concentrations for Fifty Percent Inhibition (IC50) range from 0.930 mg/mL to 3.861 mg/mL. The hydroethanolic macerated extract 70% (Eeth 70%) is the most active fraction on C. albicans (CMF = 7.8125 ± 0.00 mg/mL, IC50 = 0.941 ± 0.009 mg/mL) compared to the total of the five crude extracts tested. The preliminary phytochemical screening of the five crude extracts revealed the presence of alkaloids, saponins, terpenoids steroids and tannins (catechics and gallics) at various levels of concentration in our study. Eeth 70%, the most active extract in our work, contains in medium concentrations the same active ingredients cited above. Finally, we note that the hydroethanolic macerated extract 70% is the most active fractions in this work. It may, however, subject to toxicological studies, be used in the treatment of theskin, the cutaneous appendages and the mucous membranes in humans.

68-73

Authors: VV Prasanth, Della Grace Thomas Parambi, Shashi Ranjan

Total of 8 formulations of in situ gels of Levofloxacin hydrochloride were prepared by pH triggered in situ gelling system using different polymers like sodium alginate as gelling agent, Noveon AA-1 polycarbophil and HPMC E50LV as viscosity enhancing agent and benzalkonium chloride as preservative. All the prepared formulations were clear and the visual appearance was found to be transparent. The pH of the prepared formulations was ranged between 6.50and 7.00. The drug content varied between 96.84 ± 0.396 and 99.65±0.489 % which indicated that the uniform distribution of drug was found in all the prepared formulations. Among all the formulations, the formulations A4 and A8 showed better gelling capacity. The shear rate on the preparation was large during the blinking stage. From the in vitro drug release profile the formulations A4 and A8 was selected as the best formulations and these formulations were used for further studies such as mechanism of drug release, sterility, antimicrobial efficacy, ocular irritation and accelerated stability. Both formulations provided good fit to the Higuchi model. According to this model, the drug release from these gels may be controlled by diffusion through the micro-pores. The selected formulations showed good anti-microbial action against the organisms and ocular irritation studies revealed that the selected formulations were good with non-irritation and there were no ocular damage or abnormal clinical signs. During and at the end of the accelerated stability study, the selected formulations did not undergo any chemical changes/interaction and remained stable during the study period and showed almost similar physical stability and drug content.

80-85

Authors: Chhavi Singh, Harsh Omer

Introduction: Neck disorders remain a common problem in modern world. Patients with chronic neck pain uses health care services twice as much as the population on average. The origin of neck pain can be multifactorial. Aim and objectives: To determine whether only neck muscle isometrics or neck along with shoulder muscle isometrics are more effective in relieving chronic neck pain. Methodology: 30 female subjects with mean age 20.23±1.96 yrs, have been included in the study as the sample size with 10 equal subjects assigned to each group with mean age of 20.5±2.20 in group A, 19.8±1.37 in group B, 20.4±2.24 in group C as per inclusion criteria via random sampling method. Conclusion: Results of the study shows that pain & strength of neck muscles were improved in the subjects with neck pain individually in all the groups but does not show any significant improvement among the groups. Thus, neck pain can be reduced after training periods of neck muscles and shoulder muscles with intensive strength.

94-101

Authors: Shanmugam Shanmugam, Rakesh Kumar Jat

The Diabetes Mellitus patients glucose level alteration results were shown to few extent increased Glucose level with Diabetes Mellitus (18.7 ± 0.0), Type-I Diabetes Mellitus (74.5 ± 2.74), T-II Diabetes Mellitus (76.9 ± 7.88) when make comparison with regular well fit volunteer (123.7 ± 1.953) & 40-50 years age groups of the patients were higher prevalence of Diabetes Mellitus (553 Numbers & 36.9 %). Non Vegetarian are exaggerated more numbers & percentage of Diabetes Mellitus (542 Numbers & 36.1 %) when compare to Vegetarian (958 Numbers & 63.9 %) & also prominently affected DM with professional workers (540 Numbers & 36 %). Comparatively 80-100 Kgs body weight of Diabetes Mellitus patient’s prevalence increased in Coimbatore zone. In Coimbatore zone T-I DM (470 Numbers & 31.3 %) Patients prevalence were more T-II Diabetes Mellitus Patients (396 Numbers & 26.4 %) & non smokers were very less (544 Numbers & 36.3 %). The result of inpatients indicated that theT-I Diabetes Mellitus prescriptions (228 Numbers & 15.2%) were more & also out patients of T–II Diabetes Mellitus prescription (788 Numbers & 52.5%) were more (290 Numbers & 19.4%). The T-I DM proportional statement indicated Diabetes Mellitus associated Hyperlipidemic (38 Numbers & 4.8 %), patient’s prevalence was more & also prescribed Poly therapy prescriptions (1155 Numbers & 77 %). The results of prescribed tablet formulations were present in more numbers in the prescriptions when compared to other formulations.

109-113

Authors: Shaikh Nawaj Siraj, Saleem Mau Patel, G J Khan, K I Molvi, PATEL M Siddik, Shaoor Ahmad

Oral route the most popular route of administration for systemic action .Oral conventional drug delivery has following limitation of unpredictable gastric emptying rate, short gastro intestinal transit time, and inter subject variability leads in to less bioavailability so goal of drug delivery were not properly achieved by conventional dosage forms. So there is need of sustained drug delivery. The sustained drug delivery can be achieved by matrix tablet wherein a solid drug is dispersed in an insoluble matrix. The matrix tablets can be prepared by wet granulation method or modern thermal sintering technique. Sintering concept in the pharmaceuticals technology is very novel. The term sintering means fusion of particles or formation of welded bonds between particles of polymer. Sintering is a method of heating the material in a sintering furnace below its melting point (solid-state sintering) until its particles adhere to each other. In this process, polymer particles undergo fusion or formation of welded bonds between the each particle. Controlled release oral dosage forms were developed by sintering the polymer matrix to its glass transition temperature. The use of sintering technique adds to the effectiveness of polymers to extend the release of drug from formulation depending upon the duration and temperature of sintering. Sintering technique enhanced the extent of drug retardation from the systems studied is short enough for it to be a suitable candidate for SR formulation. The term sintering means fusion of particles or formation of welded bonds between particles of polymer. The SR oral dosage forms can be developed by sintering the polymer Gastroretentive drug delivery system is facing many challenges which can be overcome by upcoming newly sintered technique. This review article explains about various aspects of sintering technique also highlighted some research work on sintered technology.