Development and characterization of letrozole-encapsulated polymeric beads for sustained release.

The study aimed to prepare and characterize biodegradable sustained-release beads of letrozole (LTZ) for treating cancerous disease. The ionotropic gelation method was used for the preparation and calcium chloride (CaCl2) was used as a gelating agent, while chitosan (CTS) and sodium alginate (NaAlg) as biodegradable polymeric matrices in the blend hydrogel beads. The beads were characterized for their size, surface morphology, drug entrapment efficiency, drug-polymer interaction and crystallinity using different analytic techniques, including optical microscopy, Scanning Electron Microscopy (SEM), UV-spectroscopy, Fourier-transform Infrared Spectroscopy (FTIR), Thermo gravimetric Analysis (TGA), Differential Scanning Calorimetry (DSC) and X-ray Diffraction Analysis (XRD) respectively. In vitro swelling studies were also applied to observe the response of these polymeric networks against different pH (at 1.2, 6.8 and 7.4 pH). The results from TGA and DSC exhibited that the components in the formulation possess better thermal stability. The XRD of polymeric networks displays a minor crystalline and significant amorphous nature. The SEM micrographs revealed that polymeric networks have uneven surfaces and grooves. Better swelling and in vitro outcomes were achieved at a high pH (6.8,7.4), which endorsed the pH-responsive characteristics of the prepared beads. Hence, beads based on chitosan and sodium alginate were successfully synthesized and can be used for the controlled release of letrozole.

Control synthesis of mesoporous silica microparticles: Optimization and in vitro cytotoxicity studies.

The current paper explains how to make mesoporous silica microparticles (MSM) by mixing water and dichloromethane. Several dichloromethane-water ratios were used to adjust the reaction mixture for the first time to easily synthesize mesoporous silica micro particles with regulated particle size. By carefully modifying the concentrations of water and dichloromethane, a higher level of consistency was achieved in the production of micro particles, i.e. to a 2:1 v/v ratio. It was discovered that variations in the dichloromethane-to-water ratios significantly affect the surface roughness and morphologies of mesoporous silica particles along with size. This is most likely because the solvent affects how quickly tetraethyl orthosilicate (TEOS) and how quickly inorganic species polymerize. In all experiments, conditions were maintained the same at 25oC temperature and 1000 rpm. Scanner electron microscopy (SEM), Fourier transform infrared (FTIR) and X-ray powder diffraction (XRD) methods were used to identify the structure of MSM. The in vitro cytotoxicity assays showed that the produced particles, which had a diameter of 1.0 m, were safe for usage in the cellular system.

RP-HPLC method to assay ethinylestradiol and drospirenone with 3D chromatograph model in fixed dose in rat plasma for pharmacokinetic study analysis.

For the simultaneous measurement of Ethinylestradiol (EE) and Drospirenone (DP) in fixed-dose combination hormones tablets, a reverse-phase high-performance liquid chromatographic (RP-HPLC) method was developed. A specific, precise and accurate RP-HPLC method was developed and validated to analyse the drugs in rat plasma. The fluorescence detection for EE was made at λ= 200-310 nm and Ultraviolet-visible (UV/Vis) detection for DP was made at 270 nm. The typical EE and DP retention times were 4.19 and 5.30 minutes, respectively. The limit of detection (LOD) and limit of detection (LOQ) for EE were 0.121 and 0.282µg/mL and LOD and LOQ for DP were 2.23 and 7.697µg/mL respectively. The regression coefficient (r2) of EE and DP were 0.9937 and 0.9913 respectively. Precision's relative standard deviation (RSD) was less than 5%. The analyte recoveries of both drugs stayed within 95% of each other. All other validation parameters adhered to ICH standards. Throughout the analytical process, the analyte was stable. The advantages of the method developed include stability under different conditions and a low limit of quantification that was in micrograms. Its applicability was confirmed by the analysis of EE and DP levels in plasma samples in a designed pharmacokinetic study in rats after oral administration.

Medicinal Plants and Nonsteroidal Anti-inflammatory Drugs (NSAIDs) in Treatment of Arthritis: A Literature Review.

Context: Arthritis is an inflammatory disease of diarthrodial joints and is associated with swollen inflamed joints, disruption of joints, and loss of integrity of articular cartilage and synovial joints. Objective: The current review intended to examine the data on the epidemiology, causes, clinical diagnosis, and prevention and control of different types of arthritis and on the use of medicinal plants in gouty arthritis. Design: The research team performed a literature review, searching relevant literature databases, including bioRxiv, medRxiv, Google Scholar, Embase, PsychINFO, and PubMed. The search terms were arthritis, diarthodial joints, use of medicinal plants in gouty arthritis, and synovial joints. Setting: The study took place in the main library of the University of Sargodha in Sargodha, Pakistan. Results: The research team identified 135 studies, and eventually 92 unique academic publications were included in the analysis. Arthritis can develop and progress in any musculoskeletal joint, and most commonly occurs in knees, hips, shoulders, and hands. Major risk factors for arthritis include age, obesity, trauma, other diseases, and smoking. Arthritis is classified into various types, including rheumatoid arthritis (RA), osteoarthritis (OA), gouty arthritis, septic arthritis, and psoriatic arthritis (PsA). RA and OA are the most common types worldwide. RA is an autoimmune disease in which the body's immune cells attack the joints. OA develops due to damage of cartilage, tissues, and joints due to age, obesity, or stress on joints. Gouty arthritis develops due to hyperuricemia; deposits of monosodium urate crystals can lead to gouty arthritis. Septic arthritis occurs due to a microbial infection in synovial joints because in synovial joints the basement membrane is absent. PsA develops due to the psoriasis-skin disease. Conclusions: The current review showed that different types of arthritis has different causes and pathogeneses. Pain in joints is a major and common symptom in all types of arthritis. Arthritis is managed pharmacologically and nonpharmacologically. Treatment is different for each class of arthritis according to its cause and symptoms.

Designing of SiO2 mesoporous nanoparticles loaded with mometasone furoate for potential nasal drug delivery: Ex vivo evaluation and determination of pro-inflammatory interferon and interleukin mRNA expression.

The main objective of the current research work was to synthesize mesoporous silica nanoparticles for controlled delivery of mometasone furoate for potential nasal delivery. The optimized sol-gel method was used for the synthesis of mesoporous silica nanoparticles. Synthesized nanoparticles were processed through Zeta sizer, SEM, TEM, FTIR, TGA, DSC, XRD, and BET analysis for structural characterization. The in vitro dissolution test was performed for the inclusion compound, while the Franz diffusion experiment was performed for permeability of formulation. For the determination of expression levels of anti-inflammatory cytokines IL-4 and IL-5, RNA extraction, reverse transcription, and polymerase chain reaction (RT-PCR) were performed. The MTT assay was also performed to determine cell viability. Synthesized and functionalized mesoporous silica nanoparticles showed controlled release of drugs. FT-IR spectroscopy confirmed the presence of the corresponding functional groups of drugs within mesoporous silica nanoparticles. Zeta sizer and thermal analysis confirmed the delivery system was in nano size and thermally stable. Moreover, a highly porous system was observed during SEM and TEM evaluation, and further it was confirmed by BET analysis. Greater cellular uptake with improved permeability characteristics was also observed. As compared to the crystalline drug, a significant improvement in the dissolution rate was observed. It was concluded that stable mesoporous silica nanoparticles with significant porosity were synthesized, efficiently delivering the loaded drug without any toxic effect.

Optimization of empagliflozin immediate release tablets (10 mg) using central composite rotatable design with response surface methodology.

Empagliflozin is a selective inhibitor of sodium glucose co-transporter II, given as mono therapy or an add-on treatment to reduce the glycated hemoglobin levels in type 2 diabetes. This work deals with designing, formulating and optimizing empagliflozin (10mg) immediate release (IR) tablets by direct compression technique using different excipients. Through central composite rotatable design (CCRD), total nine formulations (EF1-EF9) were generated by changing the composition of binder avicel PH 102® (X1) and superdisintegrant acdisol⌖ (X2). Formulation runs with in suitable weight range and powder properties were subjected to compression. The influence of interaction of excipients on friability (Y1), hardness (Y2) and disintegration (Y3) were analyzed by fitting the polynomial quadratic model with response surface methodology (RSM). Trials EF2, EF7, EF8 and EF9 exhibited acceptable tablet attributes upon physico-chemical testing. Different dissolution models were applied to observe the in vitro drug release pattern in phosphate buffer of pH 6.8. The cumulative drug release of IR tablet batches followed the Weibull kinetics with regression coefficient (r2) values of 0.983-0.992. Empagliflozin trials were exposed to accelerated storage conditions (40±2°C/ 75±5% RH) for stability testing. Shelf life period of exposed formulations were computed in range of 22 to 25 months. Keeping in view of the results, it is concluded that the employed technique of preparation and optimization are observed to be excellent for developing immediate release empagliflozin (10mg) tablets.

Nanoemulsions as novel nanocarrieres for drug delivery across the skin: In-vitro, in-vivo evaluation of miconazole nanoemulsions for treatment of Candidiasis albicans.

In the current research, attempt is made to fabricate a nanoemulsion (NE) containing an antifungal agent. The prepared formulation has been expected to enhance skin penetration. It is also studied for in vitro drug release and toxicity assessment. Spontaneous titration method was used for preparation of NE. Prepared NE were characterized for their charge, size, morphology, rheological behaviour, drug release profile, skin permeability. The drug permeation and skin irritation were investigated. The in vitro antifungal activity was inspected using the well agar diffusion method. Miconazole NE showed good penetration in the skin as compared to marketed products. SEM showed semispherical shapes of the droplets. Zeta potential and zeta sizer showed that size was in nano ranges having positive charge.

Evaluation of phytochemical, anti-oxidant and cardiac depressant effect of Rumex dentatus by using Langendorff's isolated heart apparatus.

Rumex dentatus has been used traditionally for ailment of cardiovascular diseases. The aim of the present study was to assess cardiovascular effects in isolated perfused rabbit heart. Aqueous and n-butanolic fractions were assessed for their effect on perfusion pressure (PP), force of contraction (FC) and heart rate (HR) of rabbit heart using Langendorff's method. The possible mechanisms of action of extracts/fraction were assessed with and without application of different agonist/antagonist. Phytochemical, toxicity and anti-oxidant activities were also determined. Both extracts at 1mg/mL dose produced a highly significant decrease in FC and HR but PP remained unchanged. Moreover, aqueous fraction of Rumex dentatus at 0.001mg/mL dose produced a highly significant decrease in FC and HR but no significant change in PP was observed. Atropine 10-5 M did not inhibit the cardiac depressant response of both fractions. Furthermore, both fractions blocked the positive ionotropic and chronotropic effects of adrenaline and calcium chloride. Phytochemical studies have shown the presence of some phytochemicals. Acute and sub-chronic toxicity studies demonstrated that test extracts are safe and produced no significant changes in haematological and biochemical parameters. Crude extract showed significant antioxidant activity like ascorbic acid. This study revealed that this plant have good cardiac depressant effect.

Endothelium independent calcium channel blocking pathways mediate antihypertensive effect of morus nigra.

Present study was conducted to validate the folkloric claims of morus nigra l. (moraceae) using invasive blood pressure measuring and ex vivo vasorelaxant experimental techniques. Intravenous administration of mn. Aq in 0.01-30 mg/kg doses caused significant decrease in mean arterial pressure and heart rate in fructose-induced hypertensive rats. It also showed relaxation in high k+ [80 mm] and pe (1µm) mediated aortic contraction with ec50 1.25 and 3.72mg/ml values, respectively. Vaso-relaxant effect of mn.aq was partially blocked in presence of l-name with ec50, 5.32mg/ml value, but showed concentration dependent significant inhibition of ligand gated and voltage gated ca+2 channels and intracellular ca+2 release, similar to verapamil. Findings of current study designate that aqueous fraction of m. Nigra possesses antihypertensive activity with concentration-dependent vaso-relaxant effect predominantly mediated through endothelial-independent calcium channel blocking pathways accompanied by partial involvement of endothelium-dependent nos mediated relaxation.

The Potentially Recommended Pharmacotherapy for COVID-19.

CONTEXT: A completely unique coronavirus (2019-nCoV), formally referred to as severe acute respiratory syndrome (SARS-CoV-2), appeared in China. SARS-CoV-2 is an etiological mediator of coronavirus 2 (COVID-19), characterized by pneumonic contagion in human beings. In spite of forceful suppression, this virus has spread worldwide. No specific drugs have been approved by the FDA for treating COVID-19 patients. OBJECTIVE: The study intended to examine the data from studies on clinical management of COVID-19. DESIGN: The research team performed a literature review, searching relevant literature databases. The sources of data included bioRxiv, medRxiv, Google Scholar, Embase, PsychINFO, WanFang Data, and PubMed. The search terms were treatment of the novel coronavirus, management of nCoV-19, chloroquine, and hydroxychloroquine. SETTING: The study took place in the main library of the University of Sargodha in Sargodha, Pakistan. RESULTS: The study identified 42 unique studies that had reported and confirmed over 1500 cases of nCoV-19 by April 21, 2020. The studies found that clinical management, for patients who presented with symptoms, included supportive care and control measures that comprised mechanical ventilator support and supplementary oxygen. CONCLUSIONS: There have been intensive attempts to explore drug therapy for the prophylaxis and treatment of SARS-CoV-2 infection during this COVID-19 pandemic. Several drugs have been identified which including remdesivir, two antimalarials (chloroquine and hydroxychloroquine) and immunosuppressive agents. The effects of most drug interventions are currently highly uncertain and several drugs and vaccines are under trail for the effective treatment of COVID-19 virus, until an effective treatment will discover social distancing and physical hygiene should be practiced strictly.

Antiviral activity of green silver nanoparticles produced using aqueous buds extract of Syzygium aromaticum.

In the present study, we synthesized silver (Ag) nanoparticles using aqueous extracts of clove (Syzygium aromaticum) (SAE). This synthesis of green silver nanoparticles (AgNP) was a novel and effectual tool against the Newcastle Viral Disease (NDV). Syzygium aromaticum extract was used as reducing and stabilizing agent for synthesis of silver nanoparticles. AgNP were characterized using diversity of biophysical methods inclusive of Fourier transform infrared spectroscopy (FTIR), UV-VIS spectroscopy and Transmission electron microscopy (TEM) for morphology and size. Furthermore, XRD analysis confirmed the crystalline nature of the particles. In current investigations, the antiviral activity of clove buds silver nanoparticles was inspected in-vitro and in-ovo. Embryonated chicken eggs were used to perform the cytotoxicity assay of the clove extract silver nanoparticles (CESN). CESN showed in vitro antiviral activity against NDV in embryonated eggs.

Biochemical Dynamics and Clinical Features of Novel Corona Virus (2019-nCoV).

CONTEXT: The novel Corona Virus (nCoV-19) was initially reported in Wuhan, China during December 2019, and later people with nCoV-19 were identified in different parts of the world. Infected people had shown symptoms resembling pneumonia, but about 50% of patients were asymptomatic. OBJECTIVE: The study intended to examine the data from studies on nCoV-19. DESIGN: The research team performed a literature review, searching relevant literature databases. The sources of data included bioRxiv, medRxiv, Google Scholar, Embase, PsychINFO, WanFang Data and PubMed. The search terms were novel Corona Virus, and nCoV-19 structure. SETTING: The study took place in the main library of the University of Sargodha, Sargodha, Pakistan. RESULTS: The study identified 22 studies that had reported and confirmed over 2000 cases of nCoV-19 by January 26, 2020. The studies found that the virus was transmitted through respiratory droplets. The virus has two serotypes, OC43 and 229E. CONCLUSIONS: No specific curative therapy is available for CoVid-19. However, certain precautionary measures may potentially reduce the transmission, including washing hands, using sanitizers frequently, avoiding public gatherings, and quarantining or isolating patients. This virus has spread globally and immunocompromised individuals, and especially older individuals, are at significant risk. Community and healthcare professionals have a positive role to play in controlling the spread of the disease.

Prevalence and treatment of neurological and psychiatric disorders among tertiary hospitals in Pakistan; findings and implications.

INTRODUCTION: Mental health and neurological disorders are prevalent in Pakistan. However, there are considerable concerns with their management due to issues of access, availability of trained personnel and stigma alongside paucity of such data. Consequently, there is a need to document current treatment approaches starting with tertiary hospitals in Pakistan where patients with more severe mental and neurological disorders are typically treated. Subsequently, use the findings to help direct future policies and initiatives. METHODS: Multi-centered, cross-sectional, prospective study principally evaluating current medicine usage among patients attending tertiary hospitals in Pakistan with psychiatric and neurological disorders. In addition, possible factors contributing to the prevalence of these disorders in this population to help with future care. All 23 tertiary care hospitals in the ten major Districts in Pakistan were included, which cover 75% of the population. RESULTS: 57,664 patients were evaluated of which 35.3% were females. Both females and males had multiple brain disorders and multiple co-morbidities. Schizophrenia was the most prevalent disorder overall among both females (25.2%) and males (30.4%). A median of six medicines were prescribed per patient, with antipsychotics and antidepressants the most prescribed medicines. Clozapine was the most prescribed medicine in males (12.25%) and females (11.83%) including for psychiatric disorders, with sodium valproate the most prescribed medicine in epilepsy in males (42.44% of all anti-epileptic medicines) as well as females (46.38%). There was a greater prevalence of both disorders among the lower classes. A greater prevalence of schizophrenia was seen in patients abusing alcohol and smokers. The divorce rate was higher among the studied patients and the prevalence of depression was higher among the widowed population. CONCLUSIONS: There were concerns with the quality of prescribing including the extent of polypharmacy as well as possible overuse of clozapine especially in patients with epilepsy, both of which need addressing.

Development, characterization and evaluation of anti-fungal activity of miconazole based nanogel prepared from biodegradable polymer.

Topical candidiasis is a known skin fungal infection which is usually treated by conventional dosage forms such as cream, gel, emulgel which are having numerous adverse effects on skin. To overcome such disadvantages, different novel drug delivery systems have been considered. Polymer based nano-particulate systems have shown good skin penetration after topical application. Therefore, in the present study the main focus was on the pathology, pathogenesis, and consequently topical treatment of candidiasis. Nanogel containing miconazole have been prepared from the natural polymers i.e. gelatin and chitosan. The nanogel of miconazole (100 mg) nitrate was formulated by modified emulsification-diffusion technique and characterized for different parameters. From all the seven nanogel formulations named as F1 to F7, F1 (Gelatin and Chitosan in the percentage of 82.85 and 17.15 respectively) have been selected as model formulations. The reason behind that was as per ICH stability guideline, the formulations F1 was found optimum and stable. Miconazole nanogel formulations F1 also showed the maximum release i.e. 78 % approximately. XRD showed the formulated nanogel was in crystalline shape. In summary, the miconazole nanogel drug delivery systems have two main advantages i.e. they are topical preparation as well as nano sized. It can be postulated that nanogel may be a best approach to treat the fungal skin diseases.

Pattern of inappropriate antibiotic use among hospitalized patients in Pakistan: a longitudinal surveillance and implications.

Background: The inappropriate use of antibiotics in hospitals increases resistance, morbidity, and mortality. Little is currently known about appropriate antibiotic use among hospitals in Lahore, the capital city of Pakistan. Methods: Longitudinal surveillance was conducted over a period of 2 months among hospitals in Lahore, Pakistan. Antibiotic treatment was considered inappropriate on the basis of a wrong dosage regimen, wrong indication, or both based on the British National Formulary. Results: A total of 2022 antibiotics were given to 1185 patients. Out of the total prescribed, approximately two-thirds of the study population (70.3%) had at least one inappropriate antimicrobial. Overall, 27.2% of patients had respiratory tract infections, and out of these, 62.8% were considered as having inappropriate therapy. Cephalosporins were extensively prescribed among patients, and in many cases, this was inappropriate (67.2%). Penicillins were given to 283 patients, out of which 201 (71.0%) were prescribed for either the wrong indication or dosage or both. Significant variations were also observed regarding inappropriate prescribing for several antimicrobials including the carbapenems (70.9%), aminoglycosides (35.8%), fluoroquinolones (64.2%), macrolides (74.6%) and other antibacterials (73.1%). Conclusion: Educational interventions, institutional guidelines, and antimicrobial stewardship programs need to be developed to enhance future appropriate antimicrobial use in hospitals in Pakistan. Policies by healthcare and Government officials are also needed to minimize inappropriate antibiotic use.

Impact of pharmacist's intervention on disease related knowledge, medication adherence, HRQoL and control of blood pressure among hypertensive patients.

The present study was aimed to evaluate the effect of educational intervention provided to the patients of hypertension through pharmacist with the goal to improve knowledge about hypertension, adherence to prescribed medicines, blood pressure control and HRQoL(Health Related Quality of Life).A total of 384 patients were assigned randomly into 2 groups including intervention and control groups each having 192 patients. Urdu versions of knowledge questionnaire regarding hypertension, medication adherence scale (MMAS-U) by Morisky and EuroQol scale (EQ-5D) were utilized. Each patient's blood pressure was measured. After educational intervention, an increase was found in mean knowledge score about hypertension (18.18 ± 4.00), adherence score (5.89 ± 1.90), HRQoL score (0.73 ± 0.12) and Visual Analogue Scale (VAS) score (69.39 ± 5.90) among the IG. The blood pressure control also improved and lower systolic (131.81 ± 10.98 mmHg) and diastolic blood pressures (83.75 ± 6.21 mmHg) were observed among the patients of IG. This study showed that educational programs are useful for patients in increasing patient's levels of knowledge about hypertension, improving adherence to prescribed medication and enhancing blood pressure control. This increase is in turn accountable to improve HRQoL.

Indigenous medicinal plants of Pakistan used to treat skin diseases: a review.

ETHNO-PHARMACOLOGICAL RELEVANCE: Plants are providing reliable therapy since time immemorial. Pakistan has a great diversity in medicinal flora and people use these ethno-medicines to deal with many skin problems. This review explores the fundamental knowledge on various dermatological properties of medicinal plants of Pakistan and is aimed to provide a baseline for the discovery of new plants having activities against skin issues. MATERIAL AND METHOD: A total of 244 published articles were studied using different research engines like PubMed, Google, Google-scholar and science direct. RESULTS: Review of literature revealed ethno-pharmacological use of 545 plant species, belonging to 118 families and 355 genera, to combat various skin ailments. Out of these, ten most commonly used plant species belonging to ten different families are documented in this review. It was also found out that ehno-medicines are prepared using various parts of the plants including leaves (28.32%), whole plant and roots 13.17% and 10.97% respectively, in the form of powder (23.5%) and paste (22.75%). A total of 13 endangered plant species and ten commercially important plants were recorded. CONCLUSION: Medicinal plants of Pakistan have therapeutic effects against several skin problems; however most of medicinal plants are still not evaluated scientifically to support their ethno-pharmacological claim on skin. Dermatological pathogens are recommended to study. Further, the conservational programs should be established for endangered species.

Traditional medicinal plants used for respiratory disorders in Pakistan: a review of the ethno-medicinal and pharmacological evidence.

Respiratory disorders are a common cause of malady and demise in Pakistan due to its remoteness, cold and harsh climatic conditions as well as scarce health care facilities. The people rely upon the indigenous plant resources to cure various respiratory disorders. The primary objective of this review was to assemble all available ethno-medicinal data of plants used for respiratory disorders in Pakistan. Pharmacological activity of these plants (based upon published scientific research), distribution, diversity, use, preparation methods, economical value, conservation status and various available herbal products of some plants have also been explored. This study scrutinized various electronic databases for the literature on medicinal plants used in Pakistan to treat respiratory disorders. A total of 384 species belonging to 85 families used to treat respiratory disorders in Pakistan has been documented. Cough was the disorder treated by the highest number of species (214) followed by asthma (150), cold (57) and bronchitis (56). Most of the plants belongs to Asteraceae (32) and Solanaceae family (32) followed by moraceae (17), Poaceae (13), and Amaranthaceae (13) with their habit mostly of herb (219) followed by Shrub (112) and tree (69). Traditional healers in the region mostly prepare ethno medicinal recipes from leaves (24%) and roots (11%) in the form of decoction. Among the reported conservation status of 51 plant species, 5 were endangered, 1 critically endangered, 11 vulnerable, 14 rare, 16 least concern, 3 infrequent and 1 near threatened. We found only 53 plants on which pharmacological studies were conducted and 17 plants being used in herbal products available commercially for respiratory disorders. We showed the diversity and importance of medicinal plants used to treat respiratory disorders in the traditional health care system of Pakistan. As such disorders are still causing several deaths each year, it is of the utmost importance to conduct phytochemical and pharmacological studies on the most promising species. It is also crucial to increase access to traditional medicine, especially in rural areas. Threatened species need special attention for traditional herbal medicine to be exploited sustainably.

Development and evaluation of mucoadhesive buccal tablet containing metronidazole for the treatment of periodontitis and gingivitis.

The current study was designed to evaluate mucoadhesive buccal tablet containing metronidazole (MTZ) for local action aided by Hydroxypropylmethylcellulose K4M (HPMC) and Carbopol 940® (CP) as mucoadhesive polymers with other ingredients like sodium starch glycolate (SSG), polyvinyl pyrollidone K30 (PVP) as disintegrant and binders respectively. Formulations (F1-F8) were prepared by direct compression method and characterized for different physicochemical parameters. Results showed that the average weight and friability were within USP limits. Maximum mucoadhesive time was observed for F2 (14 hr) containing moderate amount of HPMC and CP used in the study. Up most mucoadhesive strength value was observed with F3 containing highest amount of HPMC used. Results indicated that high amount of HPMC was linked with the moderate to higher mucoadhesive strength and time. Maximum swelling index was observed in F7 (191.3%). Only F1-F3 showed complete in vitro MTZ release within 3 hr. Formulations containing PVP released MTZ incompletely over time while SSG released earlier. Formulation F1 was considered best in terms of MTZ release (100.5%) with diffusion based Korsmeyer-Peppas release kinetics. Therefore, MTZ exhibiting best physicochemical characters in mucoadhesive buccal tablet was found in F1 containing HPMC and CP in amounts of 37.5 mg and 25 mg, respectively, for local action.

APPLICATION OF VARIOUS POLYMERS AND POLYMERS BASED TECHNIQUES USED TO IMPROVE SOLUBILITY OF POORLY WATER SOLUBLE DRUGS: A REVIEW.

Solubility is concerned with solute and solvent to form a homogenous mixture. If solubility of a drug is low, then usually it is difficult to achieve desired therapeutic level of drug. Most of the newly developed entities have solubility problems and encounter difficulty in dissolution. Basic aim of solubility enhancement is to achieve desired therapeutic'level of drug to produce required pharmacological response. Different techniques are being used to enhance the solubility of water insoluble drugs. These techniques include particle size reduction, spray drying, kneading method, solvent evaporation method, salt formation, microemulsions, co-solven- cy, hydrosols, prodrug approach, supercritical fluid process, hydrogel micro particles etc. Selection of solubility improving method depends on drug properties, site of absorption, and required dosage form characteristics. Variety of polymers are also used to enhance solubility of these drugs like polyethylene glycol 300, polyvinyl pyrrolidone, chitosan, ß-cyclodextrins etc.