INHIBITION OF GASTRIC DEGRADATION OF OMEPRAZOLE USING A pH-SENSITIVE POLYMER AS A BINDER IN TABLET FORMULATION

Objective: This work was aimed at formulating omeprazole tablets using afzelia gum as a binder that is capable of inhibiting the gastric degradation of the drug. Methods: Afzelia gum at different concentrations of 0, 5, 10, 15, 20 and 30% was used as a binder to formulate omeprazole tablets. The tablets were formulated by direct compression and the batches labelled F1 to F6 respectively. A batch containing 15% hydroxypropyl methylcellulose (F7) was also formulated. The tablets were characterized; and dissolution in a pH 1.2 dissolution medium over 120 min period was studied. Aliquots taken every 20 min were analyzed by ultraviolet spectrophotometry to determine the amount of drug released and not degraded. Results: Amounts of drug released and not degraded at time 120 min were 53.1%, 57.3%, 57.8%, 58.8%, 62.1%, 83.4% and 90.0% for F1 to F7 respectively. Conclusion: Afzelia gum at a concentration of 30% is suitable for use as a binder in tablet formulation of omeprazole to ensure substantial inhibition of gastric degradation of the drug.

pH-sensitive polymer-based carriers as a useful approach for oral delivery of therapeutic protein: A review

: There are many proteins and enzymes in the human body, and their dysfunction can lead to disease. The use of proteins as a drug is common in various diseases such as diabetes. Proteins are hydrophilic molecules whose spatial structure is critical to their correct function. There are different ways to the administration of proteins. Protein structures are degraded by gastric acid and enzymes in the gastrointestinal tract and have a slight ability to permeation from the gastrointestinal epithelium due to their large hydrophilic nature. Therefore, their oral use has limitations. Since the oral use of drugs is one of the best and easiest routes for patients, many studies have been done to increase the stability, penetration and ultimately increase the bioavailability of proteins through oral administration. One of the studied strategies for oral delivery of protein is the use of pH-sensitive polymer-based carriers. These carriers use different pH-sensitive polymers such as eudragit®, chitosan, dextran, and alginate. The use of pH-sensitive polymer-based carriers by protecting the protein from stomach acid (low pH) and degrading enzymes, increasing permeability, and maintaining the spatial structure of the protein leads to increased bioavailability. In this review, we focus on the various polymers used to prepare pH-sensitive polymer-based carriers for the oral delivery of proteins.

Development of optimized formulation of liposome using 3-factor Box-Behnken Design

The objective of our present study is to optimize Chitosan coated liposomes formulation by Response surface methodology using 3-factor Box-Behnken Design. Different polymers based liposomes used for delivery of stable pH dependent formulation. Chitosan has been used as a pH sensitive polymer coating to target nanoparticles specifically to tumors which have a slightly acidic pH. Closed membrane system can accommodate amphiphilic or lipophilic drugs in vesicles. The optimized batch was formulated as a liposome delivery system and evaluation was done. To evaluate the unentrapped drug Shimadzu UV-Spectrometry at 228 nm was used and absorbance was noted. Response surface graph was prepared to predict value and the optimized formulation (Chitosan coated liposomes) can be used for loading of bio-active.The values of percent drug entrapment and average vesicle size were presented and found formulation F3&F5 were optimized for further evaluating on basis of particle size and drug loading.

An On-Demand pH-Sensitive Nanocluster for Cancer Treatment by Combining Photothermal Therapy and Chemotherapy

Combination therapy is considered to be a promising strategy for improving the therapeutic efficiency of cancer treatment. In this study, an on-demand pH-sensitive nanocluster (NC) system was prepared by the encapsulation of gold nanorods (AuNR) and doxorubicin (DOX) by a pH-sensitive polymer, poly(aspartic acid-graft-imidazole)-PEG, to enhance the therapeutic effect of chemotherapy and photothermal therapy. At pH 6.5, the NC systems formed aggregated structures and released higher drug amounts while sustaining a stable nano-assembly, structured with less systemic toxicity at pH 7.4. The NC could also increase antitumor efficacy as a result of improved accumulation and release of DOX from the NC system at pHex and pHen with locally applied near-infrared light. Therefore, an NC system would be a potent strategy for on-demand combination treatment to target tumors with less systemic toxicity and an improved therapeutic effect.