NANOTECHNOLOGY FOR OPHTHALMIC PREPARATIONS

Despite numerous efforts, ocular drug delivery still remains a challenge for pharmaceutical scientists. Most of the ocular diseases are treated by topical drug applications. But this suffers from poor bioavailability and other drawbacks. Budding interest in nanopharmaceuticals has generated a number of advancements throughout recent years with a focus on engineering novel applications. Nanotechnology also offers the ability to detect diseases at much earlier stages. Recent developments in ocular drug delivery system research have provided new insights into drug development. This review summarizes recent findings and applications of various nanoparticulate systems like nanospheres, nanosuspensions, microemulsions, liposome, etc in ocular drug delivery

DEVELOPMENT OF CASHEW GUM AND ITS DERIVATIVES FOR SUSTAINED RELEASED DRUG DELIVERY SYSTEM: BY RESPONSE SURFACE METHODOLOGY

The aim of the present study was to investigate the Cashew gum (CG) and its modifications for formulating the sustained release delivery system using theophylline (TH) as a model drug by varying the gum to drug ratio (1:1 and 3:1). Different formulations were designed, prepared and evaluated by employing response surface, optimal design of experimental technique using Design Expert® ver 8.0.1 software. The optimized formulation was identified and validated for its performance by using the numerical optimization technique. The matrix tablets were prepared by direct compression using CG, cross linked CG (CCG), carboxymethylated cashew gum (CMCG) and carboxymethylated cross linked CG (CMCCG). The modifications in CG were confirmed using FT-IR and C[13] NMR. SEM was used to study the surface morphology of formulations. In vitro drug release, gum erosion and hydration studies were carried out using a dissolution apparatus (USP 1) for 12 h using specified buffer solutions (pH 1.2 and pH 6.8). The kinetic analysis of dissolution data showed a good fit in Peppas equation which confirmed anomalous non-fickian release mechanism for CCG (epichlorhydrin/ gum ratio (E/Gb = 0.15)) with TH. The physiochemical changes, solubility, metallic remains after purification, stability of crude and purified CG and the effects of crosslinking density on swelling were also accessed. The stability of the optimized formulation indicated that it was stable. Thus, it can be concluded that CG crosslinking (E/Gb = 0.15) can be effectively employed to formulate sustained release systems

IMPROVEMENT AND ESTIMATION OF ORALLY DISINTEGRATING TABLETS CONTAINING PILOCARPINE 2-HYDROXY PROPYL β-CYCLODEXTRIN INCLUSION COMPLEX BY RESPONSE SURFACE METHODOLOGY

Objective: The study aimed to develop and evaluate an orally disintegrating tablet that contains pilocarpine and 2-hydroxy propyl β-cyclodextrin as an inclusion complex that is prepared by lyophilization used for treatment for dry mouth. Pilocarpine is utilized to treat dry mouth disorder. The inclusion complex lowers the taste of pilocarpine through the oral mucosa by the use of 2-hydroxy propyl β-cyclodextrin. Methods: The in vitro release from the insertion complex is also been studied. The parameters like differential scanning calorimetry (DSC), Fourier transformer infrared spectroscopy (FTIR), X-ray diffraction (XRD), and morphological study have been evaluated. The design of an experiment is carried out based on the concentration of croscarmellose sodium (CCS) and microcrystalline cellulose (MCC). Evaluation of the prepared orally disintegrating tablets have been carried out by different test methods like weight variation, thickness, drug content, disintegration, and in vitro dissolution study. Results: Orally disintegrating tablets are studied by utilizing the immediate pressure technique. Pilocarpine indicates the anhydrous crystalline medication, displaying sharp endothermic top at 120.2 °C, bend of 2-HPβCD demonstrates an exceptionally wide endothermal wonder among 55-100 °C for DSC. In pilocarpine spectra, characteristic band of aromatic C-H stretch at 3277 cm-1, C=C stretching at 1608 cm-1, C-N stretching at 1445 cm-1 and methoxy (CH3-O-) stretch at 2921 cm-1 was observed. The investigation shows that tablet hardness of 4.3N, breaking downtime of 12 sec and mean disintegration time is 1.562 min. Conclusion: The different diluents and super disintegrating have been applied for the quick elevation of dry mouth that helps us for patient compliance

SILVER NANOPARTICLES AND COCONUT OIL INCORPORATED BIOPOLYMER BASED ELECTROSPUN NANOFIBERS FOR WOUND DRESSING

Objective: The main aim of this study was to develop and evaluate the nanofiber loaded with coconut oil and silver nanoparticles (Ag NPs) for the treatment of wound healing by the electrospun method. Methods: The nanofibers have been created using the reduced form of silver nanoparticles and coconut oil along with Eudragit L-100 by the electrospun method. The presence of coconut oil and chemical interaction was determined by the FTIR method. XRD was made to evaluate the crystalline nature of AgNPs and Eudragit L-100. TEM was carried out to show the presence of AgNPs on the surface of nanofibers and SEM represents the diameter of the fiber. The antibacterial activity of nanofibers was carried out using a disk diffusion assay. Results: The diameter of the fibers was diminished by the excess of AgNPs in the fibers, while it increases by the coconut oil concentration, enhancing the nanofiber's hydrophilicity. FTIR spectroscopy was found in the range of coconut oil at 3553 cm-1for O-H stretch, 1365 cm-1, and 1240 cm-1 for the C-O stretch of ester groups. The diffraction peaks at 2θ of 38.5°, 44.6°, and 64.7°, in the XRD spectra of nanofiber, changed with silver NP affirming the total decrease of Ag salt. The bactericidal activity has been carried out between Escherichia coli and Staphylococcus aureus showing zones of inhibition of 20.0±0.2 mm and 14.8±0.4 mm, exhibiting excellent bactericidal characteristics for wound healing. Conclusion: The formulated nanofibers were obtained to offer protection against external agents and help in the regeneration of new tissue

Designing dual inhibitors for the treatment of Alzheimer’s disease as well as Type 2 diabetes mellitus via pharmacoinformatics approach: A step towards better medication for diabetes-associated neurological disorder

Purpose: To design dual inhibitors against Alzheimer’s disease (AD) and type 2 diabetes mellitus (T2DM) via pharmacoinformatics approach.Methods: Dual Drug Candidates (DDC) were designed and explored for their molecular interaction with several AD and T2DM targets. Pterostilbene, a natural anti-T2DM compound was coupled with different cholinesterase inhibitors to design DDC. Orisis Datawarrior online property calculator  tools, Autock 4.2 and Hex 5.1 were used to investigate the potency of all DDC relative to positive controls.Results: The study found that DDC2 (pterostilbene - methylene linker -octa hydro amino phenothiazine), DDC3 (pterostilbene - ethylene linker - N-phthalimide) and DDC5 (pterostilbene - carbonyl linker - 2-methyl-4-aminoquinoline) were the most promising out of all the DDCs. DDC2 showed strong molecular interaction with most of the AD and T2DM targets, including acetylcholinesterase, butrylcholinesterase, β-secretase, receptor for advanced glycation end products and ATP sensitive potassium channel, dipeptidyl peptidase IV and sodium glucose transport protien 2. The findings also revealed the amyloid anti-aggregation potential of DDC.Conclusion: The results show that DDC3 and DDC5 significantly interfer with the primary nucleation process of β amyloid. Thus, DDC2, DDC3 and DDC5 have strong anti-T2DM and anti-AD potential. Keywords: Type 2 Diabetes Mellitus, Alzheimer’s disease, Dual drug candidate, Amyloid-beta, Pterostilben

Targeting NF-κB signaling cascades of glioblastoma by a natural benzophenone, garcinol, via in vitro and molecular docking approaches

Glioblastoma multiforme (GBM) is regarded as the most aggressive form of brain tumor delineated by high cellular heterogeneity; it is resistant to conventional therapeutic regimens. In this study, the anti-cancer potential of garcinol, a naturally derived benzophenone, was assessed against GBM. During the analysis, we observed a reduction in the viability of rat glioblastoma C6 cells at a concentration of 30 µM of the extract (p < 0.001). Exposure to garcinol also induced nuclear fragmentation and condensation, as evidenced by DAPI-stained photomicrographs of C6 cells. The dissipation of mitochondrial membrane potential in a dose-dependent fashion was linked to the activation of caspases. Furthermore, it was observed that garcinol mediated the inhibition of NF-κB (p < 0.001) and decreased the expression of genes associated with cell survival (Bcl-XL, Bcl-2, and survivin) and proliferation (cyclin D1). Moreover, garcinol showed interaction with NF-κB through some important amino acid residues, such as Pro275, Trp258, Glu225, and Gly259 during molecular docking analysis. Comparative analysis with positive control (temozolomide) was also performed. We found that garcinol induced apoptotic cell death via inhibiting NF-κB activity in C6 cells, thus implicating it as a plausible therapeutic agent for GBM

Formulation of Sustained-release diltiazem matrix tablets using hydrophilic gum blends

Purpose: To develop sustained release matrix tablets of diltiazem hydrochloride (DTZ) using karaya gum (K) alone or in combination with locust bean gum (LB) and hydroxypropyl methylcellulose (H). Methods: Matrix tablets of DTZ were prepared at different ratios of drug:gum (1:1, 1:2, and 1:4) and of the gum blends (K, K/LB, K/H and K/LB/H) by direct compression. The matrix tablets were evaluated for hardness, friability, in vitro release and drug content. The formulations were also characterised by scanning electron microscopy (SEM), Fourier transform infra-red spectroscopy (FTIR) and differential scanning calorimetry (DSC). A commercial diltiazem hydrochloride product Dilzem SR, was used as a reference for comparison. Results: Tablets with only K or K/H had the highest mean dissolution time (MDT), the least dissolution efficiency (DE, 12 %), and released drug by swelling, diffusion and erosion mechanisms. Karaya gum or combinations with locust bean gum sufficiently controlled drug release, while combinations of KH and KLBH exhibited high and low drug release efficiency, respectively. SEM images of the tablets before and after dissolution showed morphological changes on the tablet surface while FTIR and DSC studies indicate that there was no chemical interaction between the drug and the polymers. Three of the formulations compared well with the reference (p < 0.05) in terms of release characteristics. Conclusion: The results of the study demonstrate that karaya gum alone or in suitable combination with locust bean gum and hydroxypropyl methylcellulose is suitable for formulating sustained-release matrix tablets of diltiazem

Consumers' awareness, attitude and associated factors towards self-medication in Hail, Saudi Arabia.

OBJECTIVES:To determine the factors motivating the consumers towards self-medication, the intended indications and the consumers' perceptions about complications that may arise due to its use. DESIGN:Cross-sectional community based prospective study. PLACE AND DURATION OF STUDY:Community pharmacies located at various locations of Hail, Saudi Arabia from January 2019 to March 2019. METHODS:The subjects of this cross-sectional study were people visiting community pharmacies for self-medication. Data on 663 participants was collected through a validated questionnaire prepared on the basis of WHO guidelines for the regulatory assessment of medicinal products for use in self-medication. Two trained data collectors visited the randomly selected community pharmacies, approached and interviewed the consumers purchasing medicines without prescriptions. Data was entered in SPSS and analyzed using descriptive and inferential analyses (alpha level = 0.05). RESULTS:Out of 663 respondents, 68.6% were university graduates; and 33.9% were healthcare professionals. Consumers preferred self-medication mainly for headache (85.8%), cold and sore throat (80.8%), cough (75.7%) and fever (71.8%) with the justification that these illnesses were minor (90.2%), time saving (82.2%), convenient (74.7%), quicker relief (66.1%), and economical (61.2%). Occupation was significantly associated with the reasons for preferring self-medication (p<0.001). Similarly, age, gender and education were also significantly associated with most of the reasons for opting self-medication. People were quite aware about harmful consequences of self-medication. Multivariate logistic regression analysis showed that the respondents with lower education (AOR = 2.404 [95% CI: 1.579-3.661]), non-healthcare professionals (AOR = 1.712 [95% CI: 1.143-2.565]) and higher monthly income (AOR = 0.376 [95% CI: 0.236-0.599]) preferred self-medication (p <0.001, p = 0.009, p <0.001) respectively. CONCLUSION:Self-medication was prevalent among young university graduate males for minor ailments mainly due to convenience and time saving. Despite people beliefs about the harmful consequences of self-medication, its use was omnipresent particularly among the respondents with lower education, non-healthcare professionals and people with higher monthly income