Colon related diseases is the worldwide health problem in which Colorectal cancer is the second m... more Colon related diseases is the worldwide health problem in which Colorectal cancer is the second most dangerous type of cancer, affecting both men and women. The modern diet and lifestyles, with high meat consumption and excessive alcohol use, along with limited physical activity has led to an increasing mortality rate for colon cancer worldwide. As a result, there is a need to develop novel drug therapies for colon related diseases. Colon specific drug delivery system (CDDS) has attracted significant attention during the past 20 years in providing several therapeutic advantages particularly for drugs that are sensitive to acidic condition and to intestinal enzymes. The colon is a site where both local and systemic delivery of drug can takes place. Oral drug delivery to treat colonic diseases encounters many problems like drug stability in the harsh environment of upper GI tract. Sustained colonic release of drugs can be useful in the treatment of nocturnal asthma, angina and arthritis while site specific release strategy is needed for local action for condition involving colonic pathologies such as ulcerative colitis, colorectal cancer and crohn's diseases. This review is focused on primary and novel drug delivery formulation and approaches for colonic drug delivery through pH sensitive system, microbially triggered system, time release system, osmotically controlled drug system, pressure dependent release system, probiotic approach, chronotropic system, Pulsincap system, prodrug approach, Enterion capsule based system, port system, CODES™ approach, COLAL-PRED approach, multiparticulate based system.
In present study, we have tried to develop the colon targeted matrix tablets of Zidovudine(AZT) h... more In present study, we have tried to develop the colon targeted matrix tablets of Zidovudine(AZT) hydrochloride for colon cancer using microbially triggered approach. Natural polysaccharide chitosan was used as a matrix forming agents for microbially triggered approach. Optimized ratio of Ethyl Cellulose, PVP-K30 and Starch different binders in varying concentration range were explored in different formulation batches. F8 batchwas found to be optimized in terms of providing higher drug release than other formulations among F1-F12 . It was seen that on increasing the concentration of binder the amount of drug release was decreased. 12% starch concentration provided the best release pattern and give maximum release upto 98.23 % till fourteen hrs.
The purpose of this study is to understand theregulatory aspects of pharmaceutical excipients and... more The purpose of this study is to understand theregulatory aspects of pharmaceutical excipients and its role in a dosage form. In earlier days, excipients were considered as inactive ingredients but with the passage of time, the pharmaceutical scientists learned that excipients are not inactive and have an impact on the manufacture, quality, safety and efficacy of drug(s) in a dosage form. The active drug can’t be administered alone and the amount of excipients in a formulation is greater than that of drug(s). Hence, excipients act as important partner in a dosage form and affect various properties viz. absorption, efficacy, safety, bioavailability, solubility, stability, dissolution etc. in a formulation. Previous data revealed that the excipients can also produce some serious adverse effects but the regulatory control regarding the use of excipients are still not clear as compared to Active Pharmaceutical Ingredients (API’s). There is a strong need of regulation and legislation for ...
International Journal of Applied Pharmaceutics, Mar 7, 2022
The total population has been developing dramatically; be that as it may, right now, the decision... more The total population has been developing dramatically; be that as it may, right now, the decisions for male contraception are restricted. This study investigates continuous explores of male contraceptives. This study article is primarily based on the thought of contraception that must be needed toward the increasing population and giving the ideal strategy to control the fertility of humans and animals. This review featured the recent oral male contraceptives that may be revolutionary products in our world as means of contraception. The audit article considers that these contraceptives are customarily utilized for their spermicidal activities and their fundamental hormones of the awkwardness for fertility and the mechanism of activity of the impact of the antifertility of contraceptives. The present study offers up-to-date data gathered on the contraceptives used for anti-fertility activity in males. The goal of this study is to spotlight the work on the anti-fertility effect of contraceptives. Therefore these products can provide options and lowering fertility would be higher than different contraceptives. This article can also assist investigators in developing the newer contraceptive preparation for anti-fertility activity in males. The innovations in this field are important to focus on current, more intense medication having a less detrimental effect on the body function and that can be administrable on its entity, less expensive, and quite reversible.
Colonic drug delivery has gained remarkable importance for the delivery of the drugs for the trea... more Colonic drug delivery has gained remarkable importance for the delivery of the drugs for the treatment of local diseases associated with the colon. To achieve successful colonic delivery, colon targeting is of prime importance. Various natural therapies, available for the treatment of colonic diseases like ulcerative colitis, Intestinal bowel syndrome, colon cancer, diverticulitis, etc., are based on natural polymers such as guar gum, pectin, dextran, chitosan, inulin, amylose, etc. Interest in these biodegradable polymers is increasing day by day because these are safe, non-toxic, and economic and are chemically compatible with the other excipients in the formulation. Non-starch, linear polysaccharides remain intact in the physiological environment of the stomach and the small intestine, but are degraded by the bacterial inhabitants of human colon which make them potentially successful in targeted delivery systems to the colon. Some of the herbs used in the treatment of colonic dis...
The present research work was to design and develop an optimized melt-in-mouth tablet dosage form... more The present research work was to design and develop an optimized melt-in-mouth tablet dosage form of an anti-allergic drug, Levocetirizine dihydrochloride by using sublimation technology. A total number of thirteen formulations were prepared as per the standard experimental design protocol using Design Expert Software (Version 7.1.6, StatEase Inc, Minneapolis, MN). Independent variables such as the amount of subliming agent –Camphor (X1) and the amount of superdisintegrantCrospovidone (X2) were optimized by application of 2-factor, 3-level Central Composite Design. The dependent variables selected were the disintegration time, wetting time, cumulative % drug release in 10 min. and water absorption ratio of the tablet. All the physical parameters of the melt-in-mouth tablets were practically within control. The mathematical relationships were generated using multiple linear regression analysis and all the polynomial equations were found to be statistically significant (P < 0.0002)...
The purpose of present investigation was to achieve successful delivery especially to colon using... more The purpose of present investigation was to achieve successful delivery especially to colon using microbially triggered, osmotically controlled approach. Prednisolone was choosen model drug for treatment of inflammatory bowel disease (IBD). Prednisolone-β-cyclodextrin complex were prepared and phase solubility study was carried out. Cellulose acetate solution containing chitosan was used to prepare semi-permeable. Face centered central composite design was employed to study the effect on independent variables (concentration of sodium chloride, polyethylene glycol, and chitosan), % cumulative release and disintegration time. Both independent variables, the proportion of chitosan (X1) and proportion of NaCl and PEG (X2) had an influence on the % drug release in both the media (buffers and buffer with rat ceacal content). Formulations were evaluated for their Preformulation parameters and found within the specified limit. Formulation code F8 and S8 were the optimized batches with an in...
The objective of this study was to develop a gastroretentive floating drug delivery system using ... more The objective of this study was to develop a gastroretentive floating drug delivery system using gas‐forming agent like sodium bicarbonate and polymer like hydroxypropyl methylcellulose. Floating tablets were prepared for minimizing the side effects of drug which are produced due to the accumulation in the body and also increases the patient compliance. Tablets were prepared by the dry granulation (slugging) technique, using polymers such as hydroxypropyl methylcellulose (HPMC K100M) and sodium carboxy methyl cellulose. Tablets were evaluated for their physical characteristics, viz., hardness, thickness, friability, weight variation, assay and floating properties. Further, tablets were evaluated for in vitro drug release characteristics for 12 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non‐Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and p...
The main objective of this study was to target zidovudine to the colon for improvement of exploit... more The main objective of this study was to target zidovudine to the colon for improvement of exploited immunity by HIV infection using microbially triggered approach. Zidovudine is an antiretroviral drug which falls under the category of nucleoside reverse transcriptase inhibitor. Sodium starch glycolate (SSG) was also used for controlling drug release in such a manner that it can provide effective control over sustained release of drug. The matrix tablets were coated with enteric polymers as Eudragit L100 and Eudragit S100 in 1:1 ratio for controlling upto 12 hrs drug release in colon. The tablets were prepared by wet granulation method. Pre-formulation and micrometric studies of the drug, polymer & physical mixture were carried out. The results of pre-formulation studies were in accordance with reported literature values. Various in vitro tests like hardness, friability, weight variation, content uniformity, dissolution and disintegration were performed. Comparing the release profile...
Oxalis corniculata Linn. (family: Oxalidaceae) is herbaceous plant found in Himalayan region of I... more Oxalis corniculata Linn. (family: Oxalidaceae) is herbaceous plant found in Himalayan region of India. The juice of this plant is traditionally used in liver disorders by Lepcha tribal people of the Sikkim and Darjeeling region in India. No scientific evidence is reported till date to prove the role of this plant in liver disorder. The present study was carried out to prove the hepatoprotective effect of hydroalcoholic extract of O. corniculata (HAEOC) in experimental albino mice in CCl induced hepatotoxicity model. Phytochemical screening 4 confirmed the presence of carbohydrates, flavanoids, glycosides, tannins and vitamin C in the extract. The present study shows a significant increase in the levels of SGPT, SGOT and serum bilirubin levels and decrease in TP levels on exposure to CCl , indicating considerable liver damage (Table 2). 4 Administration of HAEOC at dose levels (200 and 400 mg/kg) significantly (P<0.01, P<0.005) decreased the elevated level of the serum enzymes ...
Woodfordia fruticosa Kurz is a widely used medicinal herb in different South East Asian countries... more Woodfordia fruticosa Kurz is a widely used medicinal herb in different South East Asian countries since long back and plays a potential role in curing/treating various ailments/disorders like leprosy, toothache, leucorrhea, fever, dysentery, bowel disease. This review is intended to provide the currently available information on traditional usage, chemical constituents, various biological activities and its marketed preparations. The scientists or researchers working on this plant will be definitely benefitted from the information summarized in this article.
BackgroundAcknowledging population control to be an essential step for global health promotes wid... more BackgroundAcknowledging population control to be an essential step for global health promotes wide research study in the area of male contraception. Although there are a great number of synthetic contraceptives available in the market, they have plenty of adverse effects. Different potential strategies for male contraception were investigated over a long period time consisting of hormonal, chemical, and immunological interventions, although these methods showed good antifertility results with low failure rates relative to condoms.Main textThis review is based upon the concept of herbal contraceptives which are an effective method for controlling the fertility of animals and humans. This review has highlighted herbal medicinal plants and plant extracts which have been reported to possess significant antifertility action in males. The review considers those plants which are used traditionally for their spermicidal and antispermatogenic activities and imbalance essential hormones for f...
International Journal of Drug Delivery Technology, 2010
The objective of present study was to develop colon targeted drug delivery using bacterially trig... more The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher am...
Colon related diseases is the worldwide health problem in which Colorectal cancer is the second m... more Colon related diseases is the worldwide health problem in which Colorectal cancer is the second most dangerous type of cancer, affecting both men and women. The modern diet and lifestyles, with high meat consumption and excessive alcohol use, along with limited physical activity has led to an increasing mortality rate for colon cancer worldwide. As a result, there is a need to develop novel drug therapies for colon related diseases. Colon specific drug delivery system (CDDS) has attracted significant attention during the past 20 years in providing several therapeutic advantages particularly for drugs that are sensitive to acidic condition and to intestinal enzymes. The colon is a site where both local and systemic delivery of drug can takes place. Oral drug delivery to treat colonic diseases encounters many problems like drug stability in the harsh environment of upper GI tract. Sustained colonic release of drugs can be useful in the treatment of nocturnal asthma, angina and arthritis while site specific release strategy is needed for local action for condition involving colonic pathologies such as ulcerative colitis, colorectal cancer and crohn's diseases. This review is focused on primary and novel drug delivery formulation and approaches for colonic drug delivery through pH sensitive system, microbially triggered system, time release system, osmotically controlled drug system, pressure dependent release system, probiotic approach, chronotropic system, Pulsincap system, prodrug approach, Enterion capsule based system, port system, CODES™ approach, COLAL-PRED approach, multiparticulate based system.
In present study, we have tried to develop the colon targeted matrix tablets of Zidovudine(AZT) h... more In present study, we have tried to develop the colon targeted matrix tablets of Zidovudine(AZT) hydrochloride for colon cancer using microbially triggered approach. Natural polysaccharide chitosan was used as a matrix forming agents for microbially triggered approach. Optimized ratio of Ethyl Cellulose, PVP-K30 and Starch different binders in varying concentration range were explored in different formulation batches. F8 batchwas found to be optimized in terms of providing higher drug release than other formulations among F1-F12 . It was seen that on increasing the concentration of binder the amount of drug release was decreased. 12% starch concentration provided the best release pattern and give maximum release upto 98.23 % till fourteen hrs.
The purpose of this study is to understand theregulatory aspects of pharmaceutical excipients and... more The purpose of this study is to understand theregulatory aspects of pharmaceutical excipients and its role in a dosage form. In earlier days, excipients were considered as inactive ingredients but with the passage of time, the pharmaceutical scientists learned that excipients are not inactive and have an impact on the manufacture, quality, safety and efficacy of drug(s) in a dosage form. The active drug can’t be administered alone and the amount of excipients in a formulation is greater than that of drug(s). Hence, excipients act as important partner in a dosage form and affect various properties viz. absorption, efficacy, safety, bioavailability, solubility, stability, dissolution etc. in a formulation. Previous data revealed that the excipients can also produce some serious adverse effects but the regulatory control regarding the use of excipients are still not clear as compared to Active Pharmaceutical Ingredients (API’s). There is a strong need of regulation and legislation for ...
International Journal of Applied Pharmaceutics, Mar 7, 2022
The total population has been developing dramatically; be that as it may, right now, the decision... more The total population has been developing dramatically; be that as it may, right now, the decisions for male contraception are restricted. This study investigates continuous explores of male contraceptives. This study article is primarily based on the thought of contraception that must be needed toward the increasing population and giving the ideal strategy to control the fertility of humans and animals. This review featured the recent oral male contraceptives that may be revolutionary products in our world as means of contraception. The audit article considers that these contraceptives are customarily utilized for their spermicidal activities and their fundamental hormones of the awkwardness for fertility and the mechanism of activity of the impact of the antifertility of contraceptives. The present study offers up-to-date data gathered on the contraceptives used for anti-fertility activity in males. The goal of this study is to spotlight the work on the anti-fertility effect of contraceptives. Therefore these products can provide options and lowering fertility would be higher than different contraceptives. This article can also assist investigators in developing the newer contraceptive preparation for anti-fertility activity in males. The innovations in this field are important to focus on current, more intense medication having a less detrimental effect on the body function and that can be administrable on its entity, less expensive, and quite reversible.
Colonic drug delivery has gained remarkable importance for the delivery of the drugs for the trea... more Colonic drug delivery has gained remarkable importance for the delivery of the drugs for the treatment of local diseases associated with the colon. To achieve successful colonic delivery, colon targeting is of prime importance. Various natural therapies, available for the treatment of colonic diseases like ulcerative colitis, Intestinal bowel syndrome, colon cancer, diverticulitis, etc., are based on natural polymers such as guar gum, pectin, dextran, chitosan, inulin, amylose, etc. Interest in these biodegradable polymers is increasing day by day because these are safe, non-toxic, and economic and are chemically compatible with the other excipients in the formulation. Non-starch, linear polysaccharides remain intact in the physiological environment of the stomach and the small intestine, but are degraded by the bacterial inhabitants of human colon which make them potentially successful in targeted delivery systems to the colon. Some of the herbs used in the treatment of colonic dis...
The present research work was to design and develop an optimized melt-in-mouth tablet dosage form... more The present research work was to design and develop an optimized melt-in-mouth tablet dosage form of an anti-allergic drug, Levocetirizine dihydrochloride by using sublimation technology. A total number of thirteen formulations were prepared as per the standard experimental design protocol using Design Expert Software (Version 7.1.6, StatEase Inc, Minneapolis, MN). Independent variables such as the amount of subliming agent –Camphor (X1) and the amount of superdisintegrantCrospovidone (X2) were optimized by application of 2-factor, 3-level Central Composite Design. The dependent variables selected were the disintegration time, wetting time, cumulative % drug release in 10 min. and water absorption ratio of the tablet. All the physical parameters of the melt-in-mouth tablets were practically within control. The mathematical relationships were generated using multiple linear regression analysis and all the polynomial equations were found to be statistically significant (P < 0.0002)...
The purpose of present investigation was to achieve successful delivery especially to colon using... more The purpose of present investigation was to achieve successful delivery especially to colon using microbially triggered, osmotically controlled approach. Prednisolone was choosen model drug for treatment of inflammatory bowel disease (IBD). Prednisolone-β-cyclodextrin complex were prepared and phase solubility study was carried out. Cellulose acetate solution containing chitosan was used to prepare semi-permeable. Face centered central composite design was employed to study the effect on independent variables (concentration of sodium chloride, polyethylene glycol, and chitosan), % cumulative release and disintegration time. Both independent variables, the proportion of chitosan (X1) and proportion of NaCl and PEG (X2) had an influence on the % drug release in both the media (buffers and buffer with rat ceacal content). Formulations were evaluated for their Preformulation parameters and found within the specified limit. Formulation code F8 and S8 were the optimized batches with an in...
The objective of this study was to develop a gastroretentive floating drug delivery system using ... more The objective of this study was to develop a gastroretentive floating drug delivery system using gas‐forming agent like sodium bicarbonate and polymer like hydroxypropyl methylcellulose. Floating tablets were prepared for minimizing the side effects of drug which are produced due to the accumulation in the body and also increases the patient compliance. Tablets were prepared by the dry granulation (slugging) technique, using polymers such as hydroxypropyl methylcellulose (HPMC K100M) and sodium carboxy methyl cellulose. Tablets were evaluated for their physical characteristics, viz., hardness, thickness, friability, weight variation, assay and floating properties. Further, tablets were evaluated for in vitro drug release characteristics for 12 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non‐Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and p...
The main objective of this study was to target zidovudine to the colon for improvement of exploit... more The main objective of this study was to target zidovudine to the colon for improvement of exploited immunity by HIV infection using microbially triggered approach. Zidovudine is an antiretroviral drug which falls under the category of nucleoside reverse transcriptase inhibitor. Sodium starch glycolate (SSG) was also used for controlling drug release in such a manner that it can provide effective control over sustained release of drug. The matrix tablets were coated with enteric polymers as Eudragit L100 and Eudragit S100 in 1:1 ratio for controlling upto 12 hrs drug release in colon. The tablets were prepared by wet granulation method. Pre-formulation and micrometric studies of the drug, polymer & physical mixture were carried out. The results of pre-formulation studies were in accordance with reported literature values. Various in vitro tests like hardness, friability, weight variation, content uniformity, dissolution and disintegration were performed. Comparing the release profile...
Oxalis corniculata Linn. (family: Oxalidaceae) is herbaceous plant found in Himalayan region of I... more Oxalis corniculata Linn. (family: Oxalidaceae) is herbaceous plant found in Himalayan region of India. The juice of this plant is traditionally used in liver disorders by Lepcha tribal people of the Sikkim and Darjeeling region in India. No scientific evidence is reported till date to prove the role of this plant in liver disorder. The present study was carried out to prove the hepatoprotective effect of hydroalcoholic extract of O. corniculata (HAEOC) in experimental albino mice in CCl induced hepatotoxicity model. Phytochemical screening 4 confirmed the presence of carbohydrates, flavanoids, glycosides, tannins and vitamin C in the extract. The present study shows a significant increase in the levels of SGPT, SGOT and serum bilirubin levels and decrease in TP levels on exposure to CCl , indicating considerable liver damage (Table 2). 4 Administration of HAEOC at dose levels (200 and 400 mg/kg) significantly (P<0.01, P<0.005) decreased the elevated level of the serum enzymes ...
Woodfordia fruticosa Kurz is a widely used medicinal herb in different South East Asian countries... more Woodfordia fruticosa Kurz is a widely used medicinal herb in different South East Asian countries since long back and plays a potential role in curing/treating various ailments/disorders like leprosy, toothache, leucorrhea, fever, dysentery, bowel disease. This review is intended to provide the currently available information on traditional usage, chemical constituents, various biological activities and its marketed preparations. The scientists or researchers working on this plant will be definitely benefitted from the information summarized in this article.
BackgroundAcknowledging population control to be an essential step for global health promotes wid... more BackgroundAcknowledging population control to be an essential step for global health promotes wide research study in the area of male contraception. Although there are a great number of synthetic contraceptives available in the market, they have plenty of adverse effects. Different potential strategies for male contraception were investigated over a long period time consisting of hormonal, chemical, and immunological interventions, although these methods showed good antifertility results with low failure rates relative to condoms.Main textThis review is based upon the concept of herbal contraceptives which are an effective method for controlling the fertility of animals and humans. This review has highlighted herbal medicinal plants and plant extracts which have been reported to possess significant antifertility action in males. The review considers those plants which are used traditionally for their spermicidal and antispermatogenic activities and imbalance essential hormones for f...
International Journal of Drug Delivery Technology, 2010
The objective of present study was to develop colon targeted drug delivery using bacterially trig... more The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher am...
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